Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com

Immunology/Inflammation

The immune system has evolved to survey and respond appropriately to the universe of foreign pathogens, deploying an intricate repertoire of mechanisms that keep responses to host tissues in check. The immune system is typically divided into two categories--innate and adaptive. Innate immunity refers to nonspecific defense mechanisms that come into play immediately or within hours of an antigen's appearance in the body. Adaptive immunity refers to antigen-specific immune response. The antigen first must be processed and recognized, and then the adaptive immune system creates an army of immune cells specifically designed to attack that antigen. For the adaptive immune system, specificity and sensitivity are provided by a large repertoire of antigen T-cell receptors (TCRs) constructed in their extracellular domain to recognize antigenic peptide fragments restricted and presented by histocompatibility complex molecules, and coupled through intracellular domains to signal transduction modules that serve to transmit environmental cues inside the cell. Inflammation is triggered when innate immune cells detect infection or tissue injury. Pattern recognition receptors (PRRs) respond to pathogen-associated molecular patterns (PAMPs) or host-derived damage-associated molecular patterns (DAMPs) by triggering activation of NF-κB, AP1, CREB, c/EBP, and IRF transcription factors. Induction of genes encoding enzymes, chemokines, cytokines, adhesion molecules, and regulators of the extracellular matrix promotes the recruitment and activation of leukocytes. Besides resolving infection and injury, chronic inflammation is a risk factor for cancer. Immunity has a major impact on inflammatory diseases and cancer, and biologics targeting immune cells and their factors. Immunosuppressant drugs suppress, or reduce, the strength of the body’s immune system, and have been used in the treatment of organ transplantation or autoimmunine diseases. Immunomodulator drugs have contributed to the significant improvement against cancer and other related diseases.

References: [1] Sakaguchi S, et al. Immunol Cell Biol. 2012 Mar;90(3):277-87. doi: 10.1038/icb.2012.4. [2] Newton K, et al. Cold Spring Harb Perspect Biol. 2012 Mar; 4(3): a006049.

www.MedChemExpress.com 1

2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Inhibitors, Agonists, Screening Libraries www.MedChemExpress.com

Target List in Immunology/Inflammation

• Arginase 3 • STING 99

• Aryl Hydrocarbon Receptor 6 • Thrombopoietin Receptor 102

• CCR 9 • Toll-like Receptor (TLR) 104

• CD73 14

• Complement System 16

• COX 19

• CXCR 32

• FKBP 37

• FLAP 39

• Galectin 41

• Histamine Receptor 43

• IFNAR 57

• Interleukin Related 59

• IRAK 64

• MyD88 67

• NO Synthase 69

• NOD-like Receptor (NLR) 73

• PD-1/PD-L1 76

• PGE synthase 79

• Reactive Oxygen Species 82

• Salt-inducible Kinase (SIK) 95

• SPHK 97

www.MedChemExpress.com 3 Arginase

Arginase, an enzyme within the urea cycle in the liver, is also found in many other cells and tissues, including the lung. Arginase is present in 2 isoforms: arginase I, the hepatic isoform; and arginase II, the extrahepatic isoform; each of which is encoded by a distinct gene. The expression and function of arginase I in macrophages, hepatocytes, and vascular smooth muscle cells, is stimulated by lipopolysaccharide (LPS), IL-13, altered oxygen tension, and balloon dilatation of coronary arteries. The activation and expression of endothelial arginase II can also be induced by a variety of vascular insults. Arginase competitively inhibits nitric oxide synthase (NOS) via use of the common substrate L-arginine. Inhibition of arginase activity enhances a variety of parameters relevant to allergic airways disease, possibly by altering NO homeostasis. Arginase inhibition actively augments NO production and has beneficial effects on normal cardiac function and on vascular dysfunction typical of atherogenesis, aging, and erectile dysfunction, and sickle cell disease.

4 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Arginase Inhibitors & Modulators

Arginase inhibitor 1 BEC hydrochloride Cat. No.: HY-15775 Cat. No.: HY-19548A

Bioactivity: Arginase inhibitor 1 is a potent inhibitor of human arginases I Bioactivity: BEC HCl is a slow-binding and competitive Arginase II inhibitor with Ki of 0.31 μM (ph 7.5). target: Arginase II and II with IC50s of 223 and 509 nM, respectively. [1]; In vitro: BEC HCl causes significant enhancement of NO-dependent smooth muscle relaxation in this tissue. [2] BEC HCl enhances perivascular and peribronchiolar lung… Purity: 98.00% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg

CB-1158 CB-1158 Hydrochloride (INCB01158) Cat. No.: HY-101979 (INCB01158 Hydrochloride) Cat. No.: HY-101979A

Bioactivity: CB-1158 is a potent and orally bioavailable inhibitor of Bioactivity: CB-1158 Hydrochloride is a potent and orally bioavailable

arginase, with IC50s of 86 and 296 nM for recombinant human inhibitor of arginase, with IC50s of 86 and 296 nM for arginase 1 and 2, respectively. recombinant human arginase 1 and 2, respectively.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size: 5 mg, 10 mg, 25 mg

DL-Norvaline nor-NOHA acetate (2-Aminopentanoic acid) Cat. No.: HY-W010510 (Nω-hydroxy-nor-Arginine acetate) Cat. No.: HY-112885A

Bioactivity: DL-Norvaline, a derivative of L-norvaline, L-norvaline is a Bioactivity: nor-NOHA acetate is a specific and reversible arginase non-competitive inhibitor of arginase. inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism [1]. Purity: 97.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg 5 g

Piceatannol 3'-O-glucoside (Quzhaqigan) Cat. No.: HY-N2237

Bioactivity: Piceatannol 3'-O-glucoside, an active component of Rhubarb, activates endothelial nitric oxide ( NO) synthase through

inhibition of arginase activity with IC50s of 11.22 µM and 11.06 µM against arginase I and arginase II, respectively.

Purity: 99.0% Clinical Data: No Development Reported Size: 5 mg

www.MedChemExpress.com 5 Aryl Hydrocarbon Receptor AhR

Aryl Hydrocarbon Receptor (AhR or AHR or ahr or ahR) is a protein that in humans is encoded by the AHR gene. The aryl hydrocarbon receptor is a ligand-activated transcription factor involved in the regulation of biological responses to planar aromatic (aryl) hydrocarbons, and regulates xenobiotic-metabolizing enzymes such as cytochrome P450s, most notably cyp 1A1. Aryl Hydrocarbon Receptor is a member of the family of basic helix-loop-helix transcription factors. AhR binds several exogenous ligands including natural plant flavonoids, polyphenolics and indoles, as well as synthetic polycyclic aromatic hydrocarbons and dioxin-like compounds. AhR is a cytosolic transcription factor that is normally inactive, binding to several co-chaperones. Upon ligand binding to chemicals such as 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), the chaperones dissociate resulting in AhR translocating into the nucleus and dimerizing with ARNT (AhR nuclear translocator), leading to changes in gene transcription.

6 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Aryl Hydrocarbon Receptor Inhibitors & Modulators

1,4-Chrysenequinone AHR antagonist 1 (Chrysene-1,4-dione) Cat. No.: HY-111441 Cat. No.: HY-111449

Bioactivity: 1,4-Chrysenequinone, a polycyclic aromatic quinone, acts as an Bioactivity: AHR antagonist 1 is an aryl hydrocarbon receptor (AHR) activator of aryl hydrocarbon receptor ( AhR). antagonist extracted from patent WO2017202816A1, example 23, [1] has an IC50 of 39.9 nM in human cell line .

Purity: 93.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 100 mg, 250 mg 50 mg

CAY 10465 CH-223191 Cat. No.: HY-112627 Cat. No.: HY-12684

Bioactivity: CAY 10465 is a selective and high-affinity AhR agonist, with Bioactivity: CH-223191 is a potent and specific antagonist of aryl

a Ki of 0.2 nM, and shows no effect on estrogen receptor (K i hydrocarbon receptor (AhR). CH-223191 blocks the binding of TCDD to AhR with an IC of 0.03 µM. >100000 nM). 50

Purity: 98.48% Purity: 98.16% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

Diosmin FICZ Cat. No.: HY-N0178 (6-Formylindolo[3,2-b]carbazole) Cat. No.: HY-12451

Bioactivity: Diosmin is a flavonoid found in a variety of citrus fruits and Bioactivity: FICZ is a potent aryl hydrocarbon receptor (AhR) agonist with also an agonist of the aryl hydrocarbon receptor ( AhR). a Kd of 70 pM.

Purity: 98.0% Purity: 99.42% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

GNF351 Indole-3-carbinol Cat. No.: HY-102023 (I3C; 3-Indolemethanol) Cat. No.: HY-N0170

Bioactivity: GNF351 is a full aryl hydrocarbon receptor (AHR) antagonist. Bioactivity: Indole-3-carbinol (I3C) inhibits NF-κB activity and also is GNF351 competes with a photoaffinity AHR ligand for binding to an Aryl hydrocarbon receptor ( AhR) agonist, and an inhibitor

the AHR with an IC50 of 62 nM. GNF351 is minimal toxicity in of WWP1 (WW domain-containing ubiquitin E3 ligase 1). mouse or human keratinocytes [1]. Purity: 99.90% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 200 mg, 1 g

ITE L-Kynurenine Cat. No.: HY-19317 Cat. No.: HY-104026

Bioactivity: ITE is a potent endogenous agonist of aryl hydrocarbon Bioactivity: L-Kynurenine is a metabolite of the amino acid L-tryptophan.

receptor ( AhR), binding directly to AHR, with a Ki of 3 nM. L-Kynurenine is an aryl hydrocarbon receptor agonist. ITE also has immunosuppressive activity.

Purity: 99.27% Purity: 99.40% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 50 mg

www.MedChemExpress.com 7

Mivotilate PDM2 (YH439) Cat. No.: HY-100242 Cat. No.: HY-112629

Bioactivity: Mivotilate is a nontoxic, potent activator of the aryl Bioactivity: PDM2 is a selective, high-affinity aryl hydrocarbon receptor (

hydrocarbon receptor (AhR), and acts as a hepatoprotective AhR) antagonist with an Ki of 1.2±0.4 nM. agent.

Purity: 98.0% Purity: 98.88% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg

Pifithrin-α hydrobromide Skatole (Pifithrin hydrobromide; PFTα hydrobromide) Cat. No.: HY-15484 (3-Methylindole; 3-Methyl-1H-indole) Cat. No.: HY-W007355

Bioactivity: Pifithrin-α hydrobromide is a p53 inhibitor which blocks its Bioactivity: Skatole is produced by intestinal bacteria, regulates transcriptional activity and prevents cells from apoptosis. intestinal epithelial cellular functions through activating Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor aryl hydrocarbon receptors and p38 [1]. (AhR) agonist.

Purity: 98.28% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 100 mg

StemRegenin 1 Tapinarof (SR1) Cat. No.: HY-15001 (WBI 1001; Benvitimod; GSK2894512) Cat. No.: HY-109044

Bioactivity: StemRegenin 1 is a potent aryl hydrocarbon receptor ( AhR) Bioactivity: Tapinarof is a natural aryl hydrocarbon receptor ( AhR)

antagonist with IC50 of 127 nM. agonist with an EC50 of 13 nM.

Purity: 99.50% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

8 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CCR CC chemokine receptor

CCR (Chemokine receptors) are cytokine receptors found on the surface of certain cells that interact with a type of cytokine called achemokine. There have been 19 distinct chemokine receptors described in mammals. Each has a 7-transmembrane (7TM) structure and couples to G-protein for signal transduction within a cell, making them members of a large protein family of G protein-coupled receptors. Following interaction with their specific chemokine ligands, chemokine receptors trigger a flux in intracellular calcium (Ca 2+) ions (calcium signaling). This causes cell responses, including the onset of a process known as chemotaxis that traffics the cell to a desired location within the organism. Chemokine receptors are divided into different families, CXC chemokine receptors, CC chemokine receptors, CX3C chemokine receptors and XC chemokine receptors that correspond to the 4 distinct subfamilies of chemokines they bind. Specific chemokine receptors provide the portals for HIV to get into cells, and others contribute to inflammatory diseases and cancer.

www.MedChemExpress.com 9 CCR Inhibitors & Modulators

Aplaviroc AZ084 (AK 602; GSK 873140; GW 873140) Cat. No.: HY-17450 Cat. No.: HY-119217

Bioactivity: Aplaviroc, a SDP derivative, is a CCR5 antagonist, with IC50s Bioactivity: AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a K of 0.9 nM. Has potential to treat asthma of 0.1-0.4 nM for HIV-1 Ba-L, HIV-1 JRFL and HIV-1 MOKW. i [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

AZD2098 BMS-813160 Cat. No.: HY-U00064 Cat. No.: HY-109593

Bioactivity: AZD2098 is a potent and selective CC-chemokine receptor 4 Bioactivity: BMS-813160 is the first dual CCR2/CCR5 antagonist to enter

(CCR4) inhibitor with pIC50s of 7.8, 8.0, 8.0 and 7.6 for clinical development for cardiovascular. human, rat, mouse and dog respectively, used for asthma research [1] [2]. Purity: 99.85% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

BX471 BX471 hydrochloride (ZK-811752) Cat. No.: HY-12080 (ZK-811752 (hydrochloride)) Cat. No.: HY-12080A

Bioactivity: BX471 (ZK-811752) is a potent and selective non-peptide CCR1 Bioactivity: BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with K of 1 nM for antagonist with a Ki of 1 nM, and exhibits 250-fold i selectivity for CCR1 over CCR2, CCR5 and CXCR4. human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

Purity: 95.64% Purity: 98.00% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 10 mg, 50 mg

CCR1 antagonist 1 CCR1 antagonist 6 Cat. No.: HY-U00350 Cat. No.: HY-114193

Bioactivity: CCR1 antagonist 1 is an antagonist of CCR1, with Bioactivity: CCR1 antagonist 6 (compound 16q) is a chemokine receptor 1 anti-inflammatory activity. [1] (CCR1) antagonist, with an IC50 of 3 nM .

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 100 mg, 500 mg, 250 mg

CCR1 antagonist 7 CCR1 antagonist 8 Cat. No.: HY-114194 Cat. No.: HY-120588

Bioactivity: CCR1 antagonist 7 (compound 16r) is a chemokine receptor 1 Bioactivity: CCR1 antagonist 8 (compound 19n), a third azaindazole series [1] compound, is a CCR1 antagonist clinical candidate, with an (CCR1) antagonist, with an IC50 of 4 nM . 2+ [1] IC50 of 1.8 nM in Ca flux assay .

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 100 mg, 250 mg, 500 mg Size: 250 mg, 500 mg

10 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

CCR2 antagonist 1 CCR2-RA-[R] Cat. No.: HY-112792 Cat. No.: HY-50081

Bioactivity: CCR2 antagonist 1 is a high-affinity and long-residence-time Bioactivity: CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine CCR2 antagonist, with a K of 2.4 nM. i receptor type 2 (CCR2) with an IC50 of 103 nM.

Purity: >98% Purity: 99.36% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CCR3 antagonist 1 CCR5 antagonist 1 Cat. No.: HY-U00331 Cat. No.: HY-100261

Bioactivity: CCR3 antagonist 1 is a potent antagonist of CCR3, used for Bioactivity: CCR5 antagonist 1 is a CCR5 antagonist which can inhibit HIV the research of immunologic and inflammatory diseases. replication extracted from WO 2004054974 A2.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 20 mg Size: 1 mg, 5 mg, 10 mg

CCR6 inhibitor 1 Cenicriviroc Cat. No.: HY-112701 (TAK-652; TBR-652) Cat. No.: HY-14882

Bioactivity: CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, Bioactivity: Cenicriviroc is an orally active, dual CCR2/CCR5 antagonist,

with IC50s of 0.45 and 6 nM for monkey and human CCR6, much also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity. more selective at CCR6 over human CCR1 (IC 50, > 30000

nM), and CCR7 (IC 50, 9400 nM). CCR6 inhibitor 1 marke… Purity: 99.82% Purity: 97.09% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Cenicriviroc Mesylate DAPTA (TAK-652 Mesylate; TBR-652 Mesylate) Cat. No.: HY-14882A (D-Ala-peptide T-amide; Adaptavir) Cat. No.: HY-P1034

Bioactivity: Cenicriviroc is a dual CCR2/CCR5 antagonist, also inhibits Bioactivity: DAPTA is a synthetic peptide, functions as a viral entry both HIV-1 and HIV-2, and displays potent anti-inflammatory inhibitor by targeting selectively CCR5, and shows potent and antiinfective activity. anti-HIV activities.

Purity: 98.23% Purity: 98.73% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 25 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

GSK2239633A GW 766994 Cat. No.: HY-100183 (GW 994) Cat. No.: HY-107051

Bioactivity: GSK2239633A is a CC-chemokine receptor 4 ( CCR4) antagonist, Bioactivity: GW 766994 is a specific and oral chemokine receptor-3 which inhibits the binding of [ 125I]-TARC to human CCR4 with a (CCR3) antagonist, which has entered clinical trial for asthma and eosinophilic bronchitis. pIC50 of 7.96±0.11.

Purity: 98.05% Purity: 99.53% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 11

INCB 3284 INCB 3284 dimesylate Cat. No.: HY-15450A Cat. No.: HY-15450

Bioactivity: INCB 3284 is a potent, selective and orally bioavailable human Bioactivity: INCB 3284 dimesylate is a potent, selective and orally CCR2 antagonist, inhibiting monocyte chemoattractant bioavailable human CCR2 antagonist, inhibiting monocyte

protein-1 binding to hCCR2, with an IC50 of 3.7 nM. INCB 3284 chemoattractant protein-1 binding to hCCR2, with an IC50 of can be used in the research of acute liver failure. 3.7 nM. INCB 3284 dimesylate can be used in the research of acute liver failure. Purity: 99.30% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 10 mg, 50 mg

INCB3344 Maraviroc Cat. No.: HY-50674 (UK-427857) Cat. No.: HY-13004

Bioactivity: INCB3344 is a potent, selective and orally bioavailable CCR2 Bioactivity: Maraviroc is a selective CCR5 antagonist with activity

antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM against human HIV. (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

Purity: 99.76% Purity: 99.71% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

MK-0812 MK-0812 Succinate Cat. No.: HY-50669 Cat. No.: HY-50669A

Bioactivity: MK-0812 is a potent and selective CCR2 antagonist with low nM Bioactivity: MK-0812 Succinate is a potent and selective CCR2 antagonist affinity for CCR2. with high affinity at CCR2.

Purity: 99.75% Purity: 99.57% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

PF-4136309 RS 504393 (INCB8761) Cat. No.: HY-13245 Cat. No.: HY-15418

Bioactivity: PF-4136309 is a potent, selective, and orally bioavailable Bioactivity: RS 504393 is a selective CCR2 chemokine receptor antagonist ( CCR2 antagonist, with IC s of 5.2 nM, 17 nM and 13 nM for 50 IC50 values are 89 nM and > 100 μM for inhibition of human human, mouse and rat CCR2. recombinant CCR2 and CCR1 receptors respectively).

Purity: 99.59% Purity: 99.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg

RS102895 RS102895 hydrochloride Cat. No.: HY-18611A Cat. No.: HY-18611

Bioactivity: RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, Bioactivity: RS102895 hydrochloride is a potent CCR2 antagonist, with an IC of 360 nM, and shows no effect on CCR1. and shows no effect on CCR1. 50

Purity: >98% Purity: 98.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

12 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

SB297006 TAK-220 Cat. No.: HY-103361 Cat. No.: HY-19974

Bioactivity: SB297006 is a CCR3 antagonist, which significantly inhibits Bioactivity: TAK-220 is a selective and orally bioavailable CCR5

proliferation and neurosphere formation in CCL11-treated antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on neural progenitor cells. the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4,…

Purity: 99.77% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

TAK-779 Teijin compound 1 (Takeda 779) Cat. No.: HY-13406 Cat. No.: HY-108323

Bioactivity: TAK-779 is a potent and selective nonpeptide antagonist of Bioactivity: Teijin compound 1 is a specific CCR 2 antagonist with IC50s CCR5 and CXCR3, with a K of 1.1 nM for CCR5, and i of 24 and 180 nM in chemotaxis and binding assay,

effectively and selectively inhibits R5 HIV-1, with EC50 … respectively.

Purity: 99.73% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg

Vercirnon Vicriviroc maleate (GSK-1605786; CCX282-B; Traficet-EN) Cat. No.: HY-15724 (SCH-417690 (maleate); SCH-D (maleate)) Cat. No.: HY-17377

Bioactivity: Vercirnon is an orally bioavailable, selective, and potent Bioactivity: Vicriviroc maleate is a potent, selective, oral bioavailable

antagonist of CCR9, with an IC50 of 10 nM, used in the and CNS penetrated antagonist of CCR5, with a Ki of 2.5 nM,

research of inflammatory bowel diseases. and also inhibits HIV-1 in PBMC cells, with IC90s of 3.3 nM (JrFL), 2.8 nM (ADA-M), 1.8 nM (301657), 4.9 nM (JV1083) … Purity: 98.04% Purity: 99.41% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg

ZK756326 dihydrochloride Cat. No.: HY-101038A

Bioactivity: ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

Purity: 99.53% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 13 CD73 ecto-5′-nucleotidase, NT5E

CD73 (Ecto-5′-nucleotidase), a component of the purinergic signaling pathway, is a 70-kD glycosylphosphatidylinositol-anchored cell surface protein encoded by the NT5E gene. CD73 has both enzymatic and non-enzymatic functions in cells. As a nucleotidase, CD73 catalyzes the hydrolysis of AMP into adenosine and phosphate, and CD73-generated adenosine plays an important role in tumor immunoescape. CD73 plays a crucial role in switching on adenosinergic signaling. CD73 also functions as a signal and adhesive molecule that can regulate cell interaction with extracellular matrix components, such as laminin and fibronectin, to mediate the invasive and metastatic properties of cancers. Both the enzymatic and non-enzymatic functions of CD73 are involved in cancer-associated processes and are not completely independent of each other. Overexpression of CD73 is associated with resistance to antitumor agents. Knockdown of CD73 inhibits in vitro cell growth, cell cycle progression and cell migration in many cancers. CD73 and its associated pathways may be useful as therapeutic targets.

14 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CD73 Inhibitors & Modulators

AB-680 CD73-IN-1 Cat. No.: HY-125286 Cat. No.: HY-103695

Bioactivity: AB-680 is highly potent, reversible and selective small Bioactivity: CD73-IN-1 is an inhibitor of CD73 which can be used in the

molecule inhibitor of CD73 (an ecto-nucleotidase), with a Ki treatment of cancer extracted from patent WO 2017153952 A1, of 4.9 pM for hCD73, displays >10,000-fold selectivity over example 80. related ecto-nucleotidases CD39. Anti-tumor activity [1]. Purity: >98% Purity: 98.78% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

MethADP MethADP sodium salt (Adenosine 5'-(α,β-methylene)diphosphate) Cat. No.: HY-112502 Cat. No.: HY-112502B

Bioactivity: MethADP is a specific CD73 inhibitor. Bioactivity: MethADP (sodium salt) is a specific CD73 inhibitor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size:

PSB-12379 Cat. No.: HY-100747

Bioactivity: PSB-12379 is a potent Ecto-5'-Nucleotidase ( CD73) inhibitor

with Kis of 9.03 nM (rat) and 2.21 nM (human).

Purity: 99.99% Clinical Data: No Development Reported Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg

www.MedChemExpress.com 15 Complement System

The complement system helps or “complements” the ability of antibodies and phagocytic cells to clear pathogens from an organism. It is part of the immune system called the innate immune system that is not adaptable and does not change over the course of an individual's lifetime. The complement system consists of a number of small proteins found in the blood, in general synthesized by the liver, and normally circulating as inactive precursors (pro-proteins). When stimulated by one of several triggers, proteases in the system cleave specific proteins to release cytokines and initiate an amplifying cascade of further cleavages. The end-result of this activation cascade is massive amplification of the response and activation of the cell-killing membrane attack complex. Over 30 proteins and protein fragments make up the complement system. Three biochemical pathways activate the complement system: the classical complement pathway, the alternative complement pathway, and the lectin pathway.

16 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Complement System Inhibitors & Modulators

Avacopan BCX 1470 (CCX168) Cat. No.: HY-17627 Cat. No.: HY-50874

Bioactivity: Avacopan (CCX168) is a potent, selective and orally available Bioactivity: BCX 1470 inhibits the esterolytic activity of factor D

complement 5a receptor inhibitor with an IC50 of 0.1 nM. (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin. IC50 Value: 96 nM (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1] Target: Factor D; C1s BCX 1470(Thrombin inhibitor) is serine protease inhibitor.BCX… Purity: 99.53% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

BCX 1470 methanesulfonate C3a 70-77 Cat. No.: HY-50875 (Complement 3a (70-77)) Cat. No.: HY-P1505

Bioactivity: BCX 1470 methanesulfonate inhibits the esterolytic activity of Bioactivity: C3a (70-77) is an octapeptide corresponding to the COOH factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold terminus of C3a, exhibits the specificity and 1 to 2% biologic better, respectively, than that of trypsin. IC50 Value: 96 nM activities of C3a. (Factor D); 1.6 nM (C1s); 326 nM (Trypsin) [1] Target: Factor D; C1s BCX 1470 is serine protease inhibitor. BCX 1470 blocks… Purity: 99.43% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg

Compstatin FD-IN-1 Cat. No.: HY-P1036 Cat. No.: HY-128570

Bioactivity: Compstatinis is a 13-residue cyclic peptide, and a potent Bioactivity: FD-IN-1 (Compound 12) is a factor D ( FD) inhibitor with an inhibitor of the complement system. IC50 of 12 nM. Complement FD, a highly specific S1 serine protease, plays a central role in the alternative complement pathway of the innate immune system. FD-IN-1 also inhib…

Purity: 98.36% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 100 mg, 250 mg, 500 mg

Leukadherin-1 PMX 205 Cat. No.: HY-15701 Cat. No.: HY-110136

Bioactivity: Leukadherin-1 is a specific agonist of CR3 and the leukocyte Bioactivity: PMX 205 is a potent complement C5a receptor ( C5aR; surface integrin CD11b/CD18. CD88) antagonist.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500u g, 1 mg, 5 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

PMX 205 Trifluoroacetate SB290157 trifluoroacetate Cat. No.: HY-110136A Cat. No.: HY-101502A

Bioactivity: PMX 205 Trifluoroacetate is a potent complement C5a Bioactivity: SB290157 trifluoroacetate is a potent and selective C3a

receptor ( C5aR; CD88) antagonist. receptor antagonist with an IC50 of 200 nM.

Purity: 98.89% Purity: 99.87% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500u g, 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 17

W-54011 Cat. No.: HY-16992A

Bioactivity: W-54011 is a potent, specific, and orally active CD88 (C5a receptor) antagonist. W-54011 inhibits the binding of 125I-labeled C5a to human neutrophils with a Ki value of 2.2 nM. IC50 value: 2.2 nM (Ki) Target: CD88 (C5a receptor) in vitro: W-54011 also inhibits C5a-induced intracellular Ca2+… Purity: 98.0% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg

18 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] COX Cyclooxygenase

Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain. Drugs, like Aspirin, that inhibit cyclooxygenase activity have been available to the public for about 100 years. Two cyclooxygenase isoforms have been identified and are referred to as COX-1 and COX-2. Under many circumstances the COX-1 enzyme is produced constitutively (i.e., gastric mucosa) whereas COX-2 is inducible (i.e., sites of inflammation). Non-steroidal anti-inflammatory drugs (NSAID), such as aspirin and ibuprofen, exert their effects through inhibition of COX. The main COX inhibitors are the non-steroidal anti-inflammatory drugs (NSAIDs).

www.MedChemExpress.com 19 COX Inhibitors & Modulators

(+)-Catechin hydrate (-)-Catechin gallate Cat. No.: HY-N0355 ((-)-Catechin 3-gallate; (-)-Catechin 3-O-gallate) Cat. No.: HY-N0356

Bioactivity: (+)-Catechin hydrate inhibits cyclooxygenase-1 ( COX-1) with Bioactivity: (-)-Catechin gallate is a minor constituent in green tea catechins. (-)-Catechin gallate inhibits the activity of an IC50 of 1.4 μM. COX-1 and COX-2 enzymes.

Purity: 99.22% Purity: 99.98% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg

(-)-Epicatechin (-)-Epicatechin gallate ((-)-Epicatechol; Epicatechin; epi-Catechin) Cat. No.: HY-N0001 (ECG; Epicatechin gallate; (-)-Epicatechin 3-O-gallate) Cat. No.: HY-N0002

Bioactivity: (-)-Epicatechin inhibits cyclooxygenase-1 ( COX-1) with an Bioactivity: Epicatechin gallate inhibits cyclooxygenase-1 ( COX-1) with

IC50 of 3.2 μM. (-)-Epicatechin inhibits the IL-1β-induced an IC50 of 7.5 μM. expression of iNOS by blocking the nuclear localization of the p65 subunit of NF-κB.

Purity: 99.00% Purity: 98.57% Clinical Data: Phase 2 Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg

(S)-(+)-Ibuprofen Aceclofenac ((S)-Ibuprofen) Cat. No.: HY-78131A Cat. No.: HY-B0634

Bioactivity: (S)-(+)-Ibuprofen is the S-enantiomer of Ibuprofen. Ibuprofen Bioactivity: Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) is an anti-inflammatory inhibitor targeting COX-1 and COX-2 analog of Diclofenac. Target: COX Aceclofenac is a

with IC50 of 13 μM and 370 μM, respectively. non-steroidal anti-inflammatory drug (NSAID) analog of Diclofenac. It is used for the relief of pain and inflammation in rheumatoid arthritis, osteoarthritis and ankylosing… Purity: 99.99% Purity: 99.80% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 g, 5 g Size: 10mM x 1mL in DMSO, 1 g, 5 g

Acemetacin Acetaminophen (Paracetamol; 4'-Hydroxyacetanilide; (TVX 1322) Cat. No.: HY-B0482 4-Acetamidophenol; APAP) Cat. No.: HY-66005

Bioactivity: Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory Bioactivity: Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (

drug and a glycolic acid ester of indometacin that is a COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used cyclooxygenase inhibitor. antipyretic and analgesic drug.

Purity: 99.97% Purity: 99.69% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 5 g, 10 g 1 g, 5 g

Adelmidrol Amfenac Sodium Hydrate Cat. No.: HY-B1026 Cat. No.: HY-17479A

Bioactivity: Adelmidrol exerts important anti-inflammatory effects that are Bioactivity: Amfenac Sodium Hydrate is a COX-2 inhibitor. partly dependent on PPARγ. Adelmidrol reduces NF-κB translocation, and COX-2 expression.

Purity: 98.0% Purity: 98.65% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 10 mg, 50 mg

20 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ampiroxicam Ampyrone (CP 65703) Cat. No.: HY-17484 (4-Aminoantipyrine) Cat. No.: HY-B1398

Bioactivity: Ampiroxicam(CP65703) is a nonselective cyclooxygenase Bioactivity: Ampyrone is a reagent for glucose determination in the inhibitor uesd as anti-inflammatory drug. Target: COX presence of peroxidase and phenol. Ampiroxicam is a non-steroidal anti-inflammatory drug. It is a prodrug of piroxicam. Ampiroxicam inhibits the stretching response in mice induced by phenylbenzoquinone (PBQ) with… Purity: 97.36% Purity: 98.86% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 1 g

Asaraldehyde (Asaronaldehyde; Asaraldehyde; Aspirin 2,4,5-trimethoxy-Benzaldehyde) Cat. No.: HY-100580 (ASA; Acetylsalicylic Acid) Cat. No.: HY-14654

Bioactivity: Asarylaldehyde is a natural COX-2 inhibitor, which isolated Bioactivity: Aspirin is a non-selective and irreversible inhibitor of

from carrot ( Daucus carota L.) seeds significantly inhibits COX-1 and COX-2 with IC50s of 5 and 210 μg/mL. cyclooxygenase II (COX-2) activity at IC50 value 100 μg/mL.

Purity: 99.68% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 100 mg Size: 10mM x 1mL in DMSO, 1 g, 5 g

ATB-346 Carprofen Cat. No.: HY-15028 Cat. No.: HY-B1227

Bioactivity: ATB-346 is a novel hydrogen sulphide-releasing derivative of Bioactivity: Carprofen is a nonsteroid anti-inflammatory agent, acts as a

naproxen with markedly reduced toxicity. IC50 value: Target: multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 COX-2 ATB-346 suppressed gastric prostaglandin E(2) synthesis μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively. as effectively as naproxen, but produced negligible damage in the stomach and intestine, Unlike naproxen and celecoxib,… Purity: 98.53% Purity: 99.76% Clinical Data: Phase 1 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 100 mg

Catechin Celecoxib ((+)-Catechin; Cianidanol; Catechuic acid) Cat. No.: HY-N0898 (SC 58635) Cat. No.: HY-14398

Bioactivity: Catechin inhibits cyclooxygenase-1 ( COX-1) with an IC50 of Bioactivity: Celecoxib is a selective COX-2 inhibitor with an IC50 of 40 1.4 μM. nM.

Purity: 99.0% Purity: 99.50% Clinical Data: Phase 4 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 100 mg, 1 g

Columbin COX-2-IN-1 Cat. No.: HY-N0389 Cat. No.: HY-U00275

Bioactivity: Columbin is a diterpenoid furanolactone with anti-inflammation Bioactivity: COX-2-IN-1 is potent and slective COX-2 inhibitor with an

activity. IC50 of 3.9 μM.

Purity: 99.42% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 21

COX-2-IN-2 COX/5-LO-IN-1 Cat. No.: HY-101655 Cat. No.: HY-U00347

Bioactivity: COX-2-IN-2 is a selective and inducible COX2 inhibitor with Bioactivity: COX/5-LO-IN-1 is an inhibitor of cylooxygenase and

an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory 5-lipoxygenase, used for the research of inflammatory and compound with anti-inflammatory and analgesic activities. allergic disease states.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Deracoxib Diclofenac (SC 046; SC 46; SC 59046) Cat. No.: HY-17509 Cat. No.: HY-15036

Bioactivity: Deracoxib, a selective cyclooxygenase-2 inhibitor, is a Bioactivity: Diclofenac is a potent and nonselective anti-inflammatory

non-narcotic, non-steroidal anti-inflammatory drug (NSAID). agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM IC50 Value: 70 to 150 uM(inhibition of 3 osteosarcoma cell for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for lines) [1] Target: COX in vitro: Concentration of deracoxib ovine COX-1 and COX-2, respectively. required for 50% inhibition of cell viability (IC50) was… Purity: 99.82% Purity: 99.98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 g, 10 g

Diclofenac diethylamine Diclofenac Sodium Cat. No.: HY-15036A (GP 45840) Cat. No.: HY-15037

Bioactivity: Diclofenac diethylamine is a potent and nonselective Bioactivity: Diclofenac Sodium (GP 45840) is a potent and nonselective

anti-inflammatory agent, acts as a COX inhibitor, with IC50s anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and of 4 nM, 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively. 5.1, 0.84 μM for ovine COX-1 and COX-2, respectively.

Purity: 99.93% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 g, 10 g 5 g

Diflunisal Etodolac (MK-647) Cat. No.: HY-18342 (AY-24236) Cat. No.: HY-76251

Bioactivity: Diflunisal (MK-647) is a salicylate derivative with Bioactivity: Etodolac (AY-24236) is a non-steroidal anti-inflammatory

nonsteroidal anti-inflammatory and uricosuric properties, compound that is a non-selective inhibitor of COX (IC 50=53.5 which is used alone as an analgesic and in rheumatoid nM) arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase ( COX) Inhibitor. Purity: 99.37% Purity: 99.10% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 50 mg, 100 mg

Etoricoxib Etoricoxib D4 (MK-0663; L-791456) Cat. No.: HY-15321 (MK-0663 D4; L-791456 D4) Cat. No.: HY-15321S

Bioactivity: Etoricoxib (MK-0663) is a non steroidal anti-inflammatory Bioactivity: Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib. agent, acting as a selective and orally active COX-2 Etoricoxib is a non steroidal anti-inflammatory agent, acting

inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 as a selective and orally active COX-2 inhibitor, with IC50s in human whole blood. of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blo…

Purity: 99.92% Purity: 99.35% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 1 mg, 5 mg

22 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Fenofibric acid Fenoprofen Calcium (FNF acid) Cat. No.: HY-B0760 Cat. No.: HY-B0288A

Bioactivity: Fenofibric acid, an active metabolite of fenofibrate, is a Bioactivity: Fenoprofen Calcium is a nonsteroidal, anti-inflammatory

PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM antiarthritic agent. Target: Prostaglandin G/H synthase 1 for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also Fenoprofen is a non-steroidal anti-inflammatory, antipyretic, inhibits COX-2 enzyme activity, with an IC of 48 nM. analgesic agent advocated for use in rheumatoid arthritis, 50 degenerative joint disease, ankylosing spondylitis and gout.… Purity: 99.38% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 1 g, 5 g

Fenoprofen Calcium hydrate Firocoxib (Fenoprofen calcium salt dihydrate) Cat. No.: HY-B0288B (ML 1785713) Cat. No.: HY-14670

Bioactivity: Fenoprofen Calcium hydrate is a nonsteroidal, Bioactivity: Firocoxib(ML 1785713) is a potent and selective cyclooxygenase anti-inflammatory antiarthritic agent. Target: Prostaglandin (COX)-2 inhibitor with IC50 of 0.13 uM, 58 fold sensitivity G/H synthase 1 Fenoprofen is a non-steroidal for COX2 VSCOX1. IC50 value: 0.13 uM [1] Target: COX2 anti-inflammatory, antipyretic, analgesic agent advocated for inhibitor in vitro: Blood concentrations resulting in 50% use in rheumatoid arthritis, degenerative joint disease,… inhibition of COX-1 and COX-2 activity in vitro were 75 +/- 2… Purity: 99.35% Purity: 99.50% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg

FK 3311 Flosulide (COX-2 Inhibitor V) Cat. No.: HY-14445 (ZK 38997; CGP 28238) Cat. No.: HY-U00083

Bioactivity: FK 3311 is a selective inhibitor of COX-2; antiinflammatory Bioactivity: Flosulide is a potent and selective COX-2 inhibitor, used for agent. IC50 Value: 1.6 uM [1] Target: COX-2 Cyclooxygenase the treatment for inflammatory diseases. (COX) is an intracellular enzyme that converts arachidonic acid into prostaglandin (PG)G2 and PGH2. in vitro: The racemic mixtures and the (R)- and (S)-isomers of the 2 metabolites… Purity: 98.06% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg

Flufenamic acid Flunixin meglumine Cat. No.: HY-B1221 Cat. No.: HY-B0386

Bioactivity: Flufenamic acid is a non-steroidal anti-inflammatory agent, Bioactivity: Flunixin Meglumine is a potent inhibitor of COX used as inhibits cyclooxygenase ( COX), activates AMPK, and also analgesic agent with anti-inflammatory and antipyretic modulates ion channels, blocking chloride channels and L-type activity. Target: COX Flunixin meglumine is a potent, Ca2+ channels, modulating non-selective cation channel… non-narcotic, non-steroidal analgesic agent with anti-inflammatory and antipyretic activity. It is a potent… Purity: 99.92% Purity: 99.65% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 100 mg 1 g, 5 g

FR-188582 Gallic acid Cat. No.: HY-U00146 (3,4,5-Trihydroxybenzoic acid) Cat. No.: HY-N0523

Bioactivity: FR-188582 is a highly selective inhibitor of cyclooxygenase ( Bioactivity: Gallic acid is an antioxidant which can inhibit both COX-2.

COX)-2, with an IC50 value of 17 nM.

Purity: >98% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

www.MedChemExpress.com 23

Ginsenoside C-K Ginsenoside Rb3 (Ginsenoside K; Ginsenoside compound K) Cat. No.: HY-N0904 (Gypenoside IV) Cat. No.: HY-N0041

Bioactivity: Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits Bioactivity: Ginsenoside Rb3 is extracted from steamed Panax notoginseng. anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced

Ginsenoside C-K exhibits an inhibition against the activity of NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T CYP2C9 and CYP2A6 in human liver microsomes with IC50s of cell lines. Ginsenoside Rb3 also inhibits the induction of 32.0±3.6 μM and 63.6±4.2 μM, respectively. COX-2 and iNOS mRNA. Purity: 98.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg

Ginsenoside Rd Ginsenoside Rg3 (Gypenoside VIII) Cat. No.: HY-N0043 (20(S)-Ginsenoside-Rg3; Rg3; S-Ginsenoside Rg3) Cat. No.: HY-N0603

Bioactivity: Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional Bioactivity: Ginsenoside Rg3 is the main component of Red ginseng. + activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rg3 inhibits Na and hKv1.4 channel with IC Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. 50s of 32.2±4.5 and 32.6±2.2 μM, respectively. Ginsenoside Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside… Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2<… Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Ginsenoside Rg5 Guaiacol Cat. No.: HY-N0908 (2-Methoxyphenol) Cat. No.: HY-N1380

Bioactivity: Ginsenoside Rg5 is the main component of Red ginseng. Bioactivity: Guaiacol, a phenolic compound isolated from Guaiac resin, Ginsenoside blocks binding of IGF-1 to its receptor with an inhibits LPS-stimulated COX-2 expression and NF-κB [1] [1] IC50 of ~90 nM. Ginsenoside Rg5 also inhibits the mRNA activation . Anti-inflammatory activity . expression of COX-2 via suppression of the DNA binding activities of NF-κB p65. Purity: 99.36% Purity: 99.29% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 100 mg

Hexahydrocurcumin Ibuprofen Cat. No.: HY-N0929 ((±)-Ibuprofe) Cat. No.: HY-78131

Bioactivity: Hexahydrocurcumin is a natural compound which posesses Bioactivity: Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 anticancer and anti-inflammatory activities; selective COX-2 and COX-2 with IC50 of 13 μM and 370 μM, respectively. inhibitor. IC50 value: Target: in vitro: The relative antioxidant potencies of ginger compounds decreased in similar order of 1-dehydro-[6]-gingerdione,… Purity: 98.58% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 1 g, 5 g

Iguratimod Indobufen (T614) Cat. No.: HY-17009 (Ibustrin) Cat. No.: HY-18763

Bioactivity: Iguratimod is an antirheumatic agent, acts as an inhibitor of Bioactivity: Indobufen is a platelet aggregation inhibitor. Indobufen is a

COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect reversible platelet cyclooxygenase ( Cox) activity inhibitor. on COX-1. Iguratimod also inhibits macrophage migration Indobufen suppresses thromboxane A 2 (TxA 2) synthes…

inhibitory factor ( MIF) with an IC50 of 6.81 μM. Purity: 99.85% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg

24 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Indomethacin Inulicin (Indometacin) Cat. No.: HY-14397 (1-O-Acetylbritannilactone) Cat. No.: HY-N0896

Bioactivity: Indomethacin is a potent and nonselective inhibitor of COX1 Bioactivity: Inulicin (1-O-Acetylbritannilactone) is an active compound isolated from Inula Britannica L. Inulicin and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. (1-O-Acetylbritannilactone) inhibits VEGF-mediated activation of Src and FAK. Inulicin (1-O-Acetylbritannilactone)

inhibits LPS-induced PGE2 production and COX-2 expression,… Purity: 98.0% Purity: 99.38% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg

Isoorientin Jaceosidin (Homoorientin) Cat. No.: HY-N0767 Cat. No.: HY-N0831

Bioactivity: Isoorientin is a potent inhibitor of COX-2 with an IC50 value Bioactivity: Jaceosidin is a flavonoid isolated from Artemisia vestita, of 39 μM. induces apoptosis in cancer cells, activates Bax and down-regulates Mcl-1 and c-FLIP expression [1]. Jaceosidin exhibits anti-cancer [2], anti-inflammatory activiti…

Purity: 99.24% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg

Ketoprofen Ketorolac (RP-19583) Cat. No.: HY-B0227 (RS37619) Cat. No.: HY-B0580

Bioactivity: Ketoprofen (RP-19583) is a non-steroidal antiinflammatory Bioactivity: Ketorolac is a non-steroidal anti-inflammatory agent, acting

agent, acting as a potent inhibitor of COX, with IC50s of 2 as a nonselective COX inhibitor, with IC50s of 20 nM for nM and 26 nM for COX-1 and COX-2 in human blood monocytes, COX-1 and 120 nM for COX-2. respectively.

Purity: 99.69% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 500 mg 1 g, 5 g

Ketorolac tromethamine salt (Ketorolac tris salt; Ketorolac Lornoxicam Tromethamine; RS37619 tromethamine salt) Cat. No.: HY-B0138 (Chlortenoxicam; Ro 13-9297; TS110) Cat. No.: HY-B0367

Bioactivity: Ketorolac tromethamine salt is a non-steroidal Bioactivity: Lornoxicam, a COX-1 and COX-2 inhibitor, is a new nonsteroidal anti-inflammatory agent, acting as a nonselective COX anti-inflammatory drug (NSAID). Target: COX Lornoxicam showed

inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2. a balanced inhibition of COX-1/-2 exhibiting the lowest IC50 (0.005 microM/0.008 microM) of the large panel of NSAIDs tested. lornoxicam showed a marked inhibition of IL-6… Purity: 99.79% Purity: 98.31% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg, 200 mg, 500 mg

Loxoprofen LY 178002 Cat. No.: HY-B0578 Cat. No.: HY-101579

Bioactivity: Loxoprofen is a non-steroidal anti-inflammatory drug. Target: Bioactivity: LY 178002 is a potent inhibitor of 5-lipoxygenase, phospholipase

COX Loxoprofen is a non-steroidal anti-inflammatory drug in A2, with IC50 of 0.6 μM for 5-1ipoxygenase, inhibits cellular the propionic acid derivatives group, which also includes production of LTB4 by human polymorphonuclear leukocytes, and ibuprofen and naproxen among others. Loxoprofen is a shows relatively weak inhibition on cyclooxygenase. non-selective cyclooxygenase inhibitor, and works by reducing… Purity: 98.82% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 25

Mefenamic acid Meloxicam Cat. No.: HY-B0574 Cat. No.: HY-B0261

Bioactivity: Mefenamic acid is a non-steroidal anti-inflammatory agent, Bioactivity: Meloxicam is a non-steroidal antiinflammatory agent, inhibits

acting as a competitive inhibitor of hCOX-1 and hCOX-2, with COX activity, with IC50s of 0.49 µM and 36.6 µM for COX-2 and IC s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively. 50 COX-1, respectively.

Purity: 99.99% Purity: 98.07% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 100 mg, 500 mg

Metamizole sodium hydrate Methyl Salicylate Cat. No.: HY-B1279 (Wintergreen oil) Cat. No.: HY-Y0189

Bioactivity: Metamizole (Dipyrone) sodium hydrate is a potent analgesic Bioactivity: Methyl Salicylate (Wintergreen oil) is a topical analgesic and drug that has been demonstrated to inhibit cyclooxygenase anti-inflammatory agent. Also used as a pesticide, a (COX). denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products [1]. A systemic acquired resista…

Purity: 98.0% Purity: 99.98% Clinical Data: Launched Clinical Data: No Development Reported Size: 500 mg Size: 10mM x 1mL in DMSO, 50 mg

Nabumetone Naproxen (BRL14777) Cat. No.: HY-B0559 ((S)-Naproxen) Cat. No.: HY-15030

Bioactivity: Nabumetone is an orally active non-acidic anti-inflammatory Bioactivity: Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 agent, acts as a potent and selective COX-2 inhibitor, and is and 5.15 μM, respectively in cell assay. the prodrug of the active metabolite 6MNA.

Purity: 99.86% Purity: 99.66% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 g, 10 g

Naproxen etemesil Naproxen sodium (LT-NS 001; MX 1094) Cat. No.: HY-19675 Cat. No.: HY-15030A

Bioactivity: Naproxen etemesil is a lipophilic, non-acidic, inactive Bioactivity: Naproxen sodium is a COX-1 and COX-2 inhibitor with IC50s of prodrug of naproxen that is hydrolysed to pharmacologically 8.72 and 5.15 μM, respectively in cell assay. active Naproxen once absorbed. Naproxen is a COX-1 and COX-2

inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay. Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 g, 10 g

Neochlorogenic acid Nepafenac (trans-5-O-Caffeoylquinic acid) Cat. No.: HY-N0722 (AHR 9434; AL 6515) Cat. No.: HY-17357

Bioactivity: Neochlorogenic acid is a natural polyphenolic compound found Bioactivity: Nepafenac(AHR 9434; AL 6515; Nevanac) is a selective COX-2 in dried fruits and other plants. Neochlorogenic acid inhibits inhibitor; is prodrug of Amfenac. IC50 value: Target: COX-2 the production of TNF-α and IL-1β. Neochlorogenic acid Nepafenac is a NSAID (nonsteroidal anti inflammatory drug) suppresses iNOS and COX-2 protein expression. Neochlorogenic that is routinely used in opthamology to control pain acid also inhibits phosphorylated NF-κB p65 and p38 MAPK… following cataract surgery. Purity: 99.46% Purity: 95.14% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

26 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Nepafenac D5 Nimesulide (AHR-9434 D5; AL-6515 D5) Cat. No.: HY-17357S (R805) Cat. No.: HY-B0363

Bioactivity: Nepafenac D5 is the deuterium labeled Nepafenac, which is a Bioactivity: Nimesulide is a selective COX-2 inhibitor, with IC50s of 70 selective COX-2 inhibitor. nM-70 μM in a time-dependent manner, but it shows no effect on

COX-1 (IC 50 >100 μM). Nimesulide has potent anti-inflammatory, analgesic and antipyretic properties. Purity: 98.0% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 100 mg, 500 mg

Nitroflurbiprofen NS-398 (HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen) Cat. No.: HY-U00013 Cat. No.: HY-13913

Bioactivity: Nitroflurbiprofen is a cyclooxygenase ( COX) inhibitor with Bioactivity: NS-398 is a non-steroidal an-inflammatory agent with analgesic nitric oxide (NO)-donating properties, modulates the increased and antipyretic effects, and selectively inhibits intrahepatic vascular tone in portal hypertensive cirrhotic prostaglandin G/H synthase 2/cyclooxygenase 2 ( COX-2)

rats. activity, with an IC50 of 3.8 μM, and has no effect on COX-1 at 100 μM. Purity: 99.64% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

Oxaprozin Oxaprozin D4 (Oxaprozinum; Wy21743) Cat. No.: HY-B0808 (Wy-21743 D4) Cat. No.: HY-B0808S

Bioactivity: Oxaprozin is an inhibitor of both COX-1 and COX-2 with IC50s Bioactivity: Oxaprozin D4 is the deuterium labeled Oxaprozin, which is a of 2.2 μM and 36 μM for human platelet COX-1 and non-steroidal anti-inflammatory drug (NSAID). IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB.

Purity: 99.63% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg

Pamicogrel Paradol (KBT3022) Cat. No.: HY-U00175 ([6]-Gingerone; [6]-Paradol) Cat. No.: HY-14617

Bioactivity: Pamicogrel (KBT3022) is a cyclooxygenase ( COX) inhibitor. Bioactivity: Paradol is a pungent phenolic substance found in ginger and other Zingiberaceae plants. Paradol is an effective inhibitor of tumor promotion in mouse skin carcinogenesis, binds to cyclooxygenase (COX)-2 active site.

Purity: >98% Purity: 98.84% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Parecoxib Parecoxib Sodium (SC 69124) Cat. No.: HY-17474 (SC 69124A) Cat. No.: HY-17474A

Bioactivity: Parecoxib is a potent and selective COX-2 inhibitor. IC50 Bioactivity: Parecoxib is a potent and selective COX-2 inhibitor. IC50 value: Target: COX-2 in vitro: The prodrug Parecoxib as well value: Target: COX-2 in vitro: The prodrug Parecoxib as well as its active metabolite val have a specific affinity to the as its active metabolite val have a specific affinity to the cannabinoid (CB) receptor measured in CB1-expressing HEK 293 cannabinoid (CB) receptor measured in CB1-expressing HEK 293 cells and rat brain tissue [1]. in vivo: Adult male… cells and rat brain tissue [1]. in vivo: Adult male… Purity: 99.32% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 25 mg, 50 mg, 100 mg 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 27

Phenacetin Phenylbutazone (Acetophenetidin) Cat. No.: HY-B0476 Cat. No.: HY-B0230

Bioactivity: Phenacetin is a non-opioid analgesic without anti-inflammatory Bioactivity: Phenylbutazone is used as a non-steroidal anti-inflammatory properties, inhibits COX-3 activity. Target: COX Phenacetin is agent for the treatment of chronic pain, including the a pain-relieving and fever-reducing drug, Phenacetin was symptoms of arthritis. Target: Others Phenylbutazone was withdrawn from the Canadian market in June 1973 due to originally made available for use in humans for the treatment concerns regarding nephropathy. the clinical and laboratory… of rheumatoid arthritis and gout in 1949. However, when… Purity: 99.09% Purity: 98.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 500 mg

Piroxicam Prim-O-glucosylcimifugin (CP-16171) Cat. No.: HY-B0253 Cat. No.: HY-N0635

Bioactivity: Piroxicam (CP-16171) is a non-steroidal anti-inflammatory Bioactivity: Prim-O-glucosylcimifugin exerts anti-inflammatory effects

drugs, acts as a COX inhibitor, with IC50s of 47, 25 μM for through the inhibition of iNOS and COX-2 expression by through human monocyte COX-1 and COX-2, respectively. regulating JAK2/STAT3 signaling.

Purity: 99.73% Purity: 99.76% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 1 g, 5 g, 10 g

Propyphenazone Rofecoxib (4-Isopropylantipyrine; Isopropylphenazone) Cat. No.: HY-A0273 (MK 966) Cat. No.: HY-17372

Bioactivity: Propyphenazone is a pyrazolone derivative with Bioactivity: Rofecoxib is a potent, specific and orally active COX-2 anti-inflammatory, analgesic and antipyretic activity, inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human Propyphenazone-based analogues as prodrugs and selective osteosarcoma cells and Chinese hamster ovary cells, with a cyclooxygenase-2 inhibitors. TargetCOX-2 Propyphenazone is 1000-fold selectivity for COX-2 over human COX-1 (IC &… structurally related to aminophenazone it has been associated… 50 Purity: 99.94% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 250 mg 100 mg

Rutaecarpine RWJ 63556 (Rutecarpine) Cat. No.: HY-N0147 Cat. No.: HY-U00022

Bioactivity: Rutaecarpine, an alkaloid of Evodia rutaecarpa, is an inhibitor Bioactivity: RWJ 63556 is an orally active COX-2 selective/5-lipoxygenase

of COX-2 with an IC50 value of 0.28 μM. inhibitor, with anti-inflammatory activities.

Purity: 99.11% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 10 mg, 50 mg, 100 mg

S-(+)-Ketoprofen S-(+)-Marmesin ((S)-Ketoprofen; Dexketoprofen) Cat. No.: HY-B2137 ((+)-Marmesin; (S)-Marmesin) Cat. No.: HY-N2176

Bioactivity: S-(+)-Ketoprofen is a potent inhibitor of both COX-1 and Bioactivity: S-(+)-Marmesin is a natural coumarin, exhibiting COX-2/5-LOX

COX-2 with IC50s of 1.9 and 27 nM, respectively. dual inhibitory activity.

Purity: 99.95% Purity: 99.04% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 25 mg, 50 mg 100 mg

28 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

S-2474 Salicin Cat. No.: HY-19212 (D-(−)-Salicin; Salicoside) Cat. No.: HY-N0149

Bioactivity: S-2474 is an inhibitor of COX-2 and 5-lipoxygenase, with IC50s Bioactivity: Salicin is a natural COX inhibitor. of 11 nM and 27 μM for COX-2 and COX-1 in human intact cells, and used as a nonsteroidal anti-inflammatory drug.

Purity: >98% Purity: 99.60% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 500 mg, 1 g, 5 g

Salicylic acid SC-560 (2-Hydroxybenzoic acid) Cat. No.: HY-B0167 Cat. No.: HY-59105

Bioactivity: Salicylic acid inhibits cyclo-oxygenase-2 ( COX-2) activity Bioactivity: SC-560 is a potent and selective COX-1 inhibitor with an IC50 independently of transcription factor (NF-κB) activation. of 9 nM.

Purity: 98.0% Purity: 99.58% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 g, 50 g 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

SC57666 SC58451 Cat. No.: HY-U00129 Cat. No.: HY-U00239

Bioactivity: SC57666 is a selective COX2 inhibitor with an IC50 of 26 nM. Bioactivity: SC58451 is a potent and selective Cox-2 inhibitor.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Sodium Salicylate (Salicylic acid sodium salt; Sulindac 2-Hydroxybenzoic acid sodium salt) Cat. No.: HY-B0167A (MK-231) Cat. No.: HY-B0008

Bioactivity: Sodium Salicylate inhibits cyclo-oxygenase-2 ( COX-2) Bioactivity: Sulindac (MK-231) is a non-steroidal antiinflammatory agent, activity independently of transcription factor (NF-κB) acts as a COX-2 inhibitor, and inhibits overexpression of activation. COX-2.

Purity: 99.93% Purity: 99.46% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 g, 50 g 100 mg, 500 mg

Syringaldehyde Tenidap Cat. No.: HY-N1390 (CP-66248) Cat. No.: HY-105028

Bioactivity: Syringaldehyde is a polyphenolic compound belonging to the Bioactivity: Tenidap, a non-steroidal anti-inflammatory drug, is a

group of flavonoids and is found in different plant species selective COX-1 inhibitor, with IC50 values of 0.03 µM and [1] like Manihot esculenta and Magnolia officinalis . 1.2 µM for COX-1 and COX-2, respectively. Tenidap has Syringaldehyde moderately inhibits COX-2 activity with… anti-inflammatory and antirheumatic properties [1] [2]. Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg

www.MedChemExpress.com 29

Tenoxicam TFAP (Ro-12-0068) Cat. No.: HY-B0440 (N-(5-Aminopyridin-2-yl)-4-(trifluoromethyl)benzamide) Cat. No.: HY-112731

Bioactivity: Tenoxicam (Ro-12-0068), an antiinflammatory agent with Bioactivity: TFAP is a selective cyclooxygenase-1 (COX-1) inhibitor, with analgesic and antipyretic properties. an IC50 of 0.8 μM.

Purity: 99.83% Purity: 99.97% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg

Thioflosulide Tilmacoxib (L-745337) Cat. No.: HY-19217 (JTE522; JTP19605; RWJ57504) Cat. No.: HY-U00197

Bioactivity: Thioflosulide (L-745337) is a selective cyclooxygenase-2 Bioactivity: Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC of 85 nM in (COX2) inhibitor, with an IC50 of 2.3 nM, and shows 50 anti-inflammatory activity. an enzyme assay.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

Timegadine Tolfenamic Acid (SR1368) Cat. No.: HY-100125 (GEA 6414) Cat. No.: HY-B0335

Bioactivity: Timegadine, a new antiinflammatory agent, is found to be a Bioactivity: Tolfenamic Acid (GEA 6414) is a non-steroidal potent, competitive inhibitor of cyclo-oxygenase ( COX) and anti-inflammatory and anti-cancer agent, selectively inhibits

lipo-oxygenase, with IC50s ranging from 5 nM (washed rabbit COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated platelets) to 20 μM (rat brain) for COX and 100 μM for (COX-2) canine DH82 monocyte/macrophage cells, but shows no lipo-oxygenase both in the cytosol fraction of horse platelet… effect on COX-1. Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 1 g, 10 g

Tolmetin sodium dihydrate Triflusal Cat. No.: HY-B1489 Cat. No.: HY-B0531

Bioactivity: Tolmetin sodium dihydrate is a non-steroidal antiinflammatory Bioactivity: Triflusal irreversibly inhibits the production of agent, and acts as a non-selective COX inhibitor. thromboxane-B2 in platelets by acetylating cycloxygenase-1. Target: COX Triflusal at 10 mM, 100 mM and 1 M decreases LDH efflux in rat brain slices after anoxia/reoxygenation by 24%, 35% and 49% respectively. Triflusal also reduces inducible NO… Purity: 99.77% Purity: 99.66% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg, 50 mg

Valdecoxib Veratric acid (SC 65872) Cat. No.: HY-15762 (3,4-Dimethoxybenzoic acid) Cat. No.: HY-N2007

Bioactivity: Valdecoxib is a highly potent and selective inhibitor of Bioactivity: Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active

COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, phenolic compound derived from vegetables and fruits, has [1] [3] respeceively. Valdecoxib can be used in the research of antioxidant and anti-inflammatory activities . arthritis and pain. Veratric acid also acts as a protective agent agai…

Purity: 99.91% Purity: 99.99% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 100 mg

30 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Xanthohumol Zaltoprofen Cat. No.: HY-N1067 (CN100) Cat. No.: HY-B0619

Bioactivity: Xanthohumol is one of the principal flavonoids isolated from Bioactivity: Zaltoprofen(CN100) is an inhibitor of COX for treatment of hops, the inhibitor of diacylglycerol acetyltransferase ( arthritis. Target: COX Zaltoprofen, a preferential COX-2 DGAT), COX-1 and COX-2, and shows anti-cancer and inhibitor, exhibited a potent inhibitory action on the anti-angiogenic activities. nociceptive responses induced by a retrograde infusion of bradykinin into the right common carotid artery in rats.… Purity: 99.68% Purity: 99.09% Clinical Data: Phase 1 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 31 CXCR CXC chemokine receptors;C-X-C motif chemokine receptors

CXCRs (CXC chemokine receptors) are integral membrane proteins that specifically bind and respond to cytokines of the CXC chemokine family. They represent one subfamily of chemokine receptors, a large family of G protein-linked receptors that are known as seven transmembrane (7-TM) proteins, since they span thecell membrane seven times. There are currently seven known CXC chemokine receptors in mammals, named CXCR1 through CXCR7. CXCR1 and CXCR2 are closely related receptors that recognize CXC chemokines that possess an E-L-R amino acid motif immediately adjacent to their CXC motif. CXCR3 is expressed predominantly on T lymphocytes. CXCR4 is the receptor for a chemokine known as CXCL12 (or SDF-1) and, as with CCR5, is utilized by HIV-1 to gain entry into target cells. The chemokine receptor CXCR5 is selectively expressed on B cells and is involved in lymphocyte homing and the development of normal lymphoid tissue. CXCR6 was formerly called three different names (STRL33, BONZO, and TYMSTR) before being assigned CXCR6 based on its chromosomal location and its similarity to other chemokine receptors in its gene sequence. CXCR7 was originally called RDC-1 (an orphan receptor) but has since been shown to cause chemotaxis in T lymphocytes in response to CXCL12 (the ligand for CXCR4) prompting the renaming of this molecule as CXCR7.

32 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] CXCR Inhibitors & Modulators

ALX 40-4C ALX 40-4C Trifluoroacetate Cat. No.: HY-P7061 Cat. No.: HY-P7061A

Bioactivity: ALX 40-4C is a small peptide inhibitor of the chemokine Bioactivity: ALX 40-4C Trifluoroacetate is a small peptide inhibitor of the chemokine receptor CXCR4, inhibits SDF-1 from binding receptor CXCR4, inhibits SDF-1 from binding CXCR4 with a Ki CXCR4 with a K of 1 μM, and suppresses the replication of X4 of 1 μM, and suppresses the replication of X4 strains of i HIV-1; ALX 40-4C Trifluoroacetate also acts as an antagon… strains of HIV-1; ALX 40-4C Trifluoroacetate also acts as…

Purity: >98% Purity: 98.15% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

AMD 3465 AMD 3465 hexahydrobromide (GENZ-644494) Cat. No.: HY-15971A (GENZ-644494 hexahydrobromide) Cat. No.: HY-15971

Bioactivity: AMD 3465 is a potent antagonist of CXCR4, inhibits binding of Bioactivity: AMD 3465 hexahydrobromide is a potent antagonist of CXCR4, AF647 AF647 12G5 mAb and CXCL12 to CXCR4, with IC50s of 0.75 nM inhibits binding of 12G5 mAb and CXCL12 to CXCR4, with IC s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the 50 replication of X4 HIV strains ( IC : 1-10 nM), but has… 50 potently inhibits the replication of X4 HIV strains ( IC50 Purity: >98% Purity: 98.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg

AMG 487 ATI-2341 Cat. No.: HY-15319 Cat. No.: HY-P0172

Bioactivity: AMG 487 is an orally active and selective antagonist of CXC Bioactivity: ATI-2341 is a CXCR4 agonist, induces CXCR4-dependent calcium chemokine receptor 3 (CXCR3) which inhibits the binding of flux, with an EC50 of 194 nM in CCRF-CEM cells. ATI-2341 is CXCL10 and CXCL11 to CXCR3 with IC s of 8.0 and 8.2 nM, 50 also a potent and efficacious mobilizer of bone marrow respectively. hematopoietic cells [1]. Purity: 99.65% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

AZD-5069 AZD8797 Cat. No.: HY-19855 Cat. No.: HY-13848

Bioactivity: AZD-5069 is a potent CXCR2 chemokine receptor antagonist, Bioactivity: AZD8797 is an allosteric non-competitive modulator of the

used for caner treatment. human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively.

Purity: 99.92% Purity: 98.22% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Baohuoside I Burixafor hydrobromide (Icariin-II; Icariside-II) Cat. No.: HY-N0011 (TG-0054 hydrobromide) Cat. No.: HY-19867A

Bioactivity: Baohuoside I, a flavonoid isolated from Epimedium koreanum Bioactivity: Burixafor hydrobromide (TG-0054 hydrobromide) is an orally Nakai, acts as an inhibitor of CXCR4, downregulates CXCR4 bioavailable and potent antagonist of CXCR4 and a well water expression, induces apoptosis and shows anti-tumor activity. soluble anti-angiogenic drug that is of potential value in treating choroid neovascularization [1]. Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal Purity: 98.96% Purity: stem…>98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

www.MedChemExpress.com 33

CXCR2-IN-1 CXCR7 modulator 2 Cat. No.: HY-101022 Cat. No.: HY-112154

Bioactivity: CXCR2-IN-1 is a central nervous system penetrant CXCR2 Bioactivity: CXCR7 modulator 2 is a modulator of C-X-C Chemokine Receptor Type 7 ( CXCR7), with a K of 13 nM. antagonists with a pIC50 of 9.3. i

Purity: 98.81% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Danirixin E6130 (GSK1325756) Cat. No.: HY-19768 Cat. No.: HY-107456

Bioactivity: Danirixin is a selective, and reversible CXCR2 antagonist, Bioactivity: E6130 is an orally available and highly selective CX3CR1

with IC50of12.5 nM for CXCL8. modulator, that may be effective for treatment of inflammatory bowel disease.

Purity: 98.21% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

IT1t IT1t dihydrochloride Cat. No.: HY-101458 Cat. No.: HY-101458A

Bioactivity: IT1t is a potent CXCR4 antagonist; inhibits CXCL12/CXCR4 Bioactivity: IT1t dihydrochloride is a potent CXCR4 antagonist; inhibits

interaction with an IC50 of 2.1 nM. CXCL12/CXCR4 interaction with an IC50 of 2.1 nM.

Purity: >98% Purity: 98.09% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

JMS-17-2 LIT-927 Cat. No.: HY-123918 Cat. No.: HY-112709

Bioactivity: JMS-17-2 is a potent and selective CX3CR1 antagonist with an Bioactivity: LIT-927 is a locally and orally active CXCL12 neutraligand [1] with anti-inflammatory effect, with a K of 267 nM for CXCL12 IC50 of 0.32 nM . i binding to its specific receptor CXCR4 [1] .

Purity: >98% Purity: 99.66% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

LY2510924 Mavorixafor Cat. No.: HY-12488 (AMD-070) Cat. No.: HY-50101

Bioactivity: LY2510924 is a potent and selective CXCR4 antagonist that Bioactivity: Mavorixafor (AMD-070) is a potent, selective and orally

blocks SDF-1 binding to CXCR4 with an IC50 of 0.079 nM. available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells … Purity: 99.91% Purity: >98% Clinical Data: Phase 2 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

34 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Mavorixafor trihydrochloride Motixafortide (AMD-070 (trihydrochloride)) Cat. No.: HY-50101A (BKT140 (4-fluorobenzoyl); BL-8040; TF14016) Cat. No.: HY-P0171

Bioactivity: Mavorixafor trihydrochloride (AMD-070 trihydrochloride) is a Bioactivity: Motixafortide (BKT140 4-fluorobenzoyl) is a novel CXCR4 potent, selective and orally available CXCR4 antagonist, with antagonist with an IC50 vakue of 1 nM. 125 an IC50 value of 13 nM against CXCR4 I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain)… Purity: 99.14% Purity: 99.19% Clinical Data: Phase 1 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 25 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

MSX-122 Navarixin Cat. No.: HY-13696 (SCH 527123; MK-7123) Cat. No.: HY-10198

Bioactivity: MSX-122 is a partial antagonist of CXCR4, inhibiting Bioactivity: Navarixin is a potent, allosteric antagonist of both CXCR1

CXCR4/CXCL12 actions, with an IC50 of 10 nM; MSX-122 has and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and anti-inflammatory and anti-metastatic activity. 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly.

Purity: 98.29% Purity: 98.62% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

NBI-74330 Nicotinamide N-oxide Cat. No.: HY-15320 Cat. No.: HY-101407

Bioactivity: NBI-74330 is a potent antagonist for CXCR3, and exhibits Bioactivity: Nicotinamide N-oxide, an in vivo nicotinamide metabolite, is a potent inhibition of ( 125I)CXCL10 and ( 125I)CXCL11 specific potent, and selective antagonist of the CXCR2 receptor.

binding with Ki of 1.5 and 3.2 nM, respectively.

Purity: 98.0% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

Plerixafor Plerixafor octahydrochloride (AMD3100 (octahydrochloride); (AMD 3100; JM3100; SID791) Cat. No.: HY-10046 JM3100 (octahydrochloride); SID791 (octahydrochloride)) Cat. No.: HY-50912

Bioactivity: Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an Bioactivity: Plerixafor octahydrochloride (AMD3100 octahydrochloride) is a selective CXCR4 antagonist with an IC of 44 nM. IC50 of 44 nM. 50

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Ethanol, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Reparixin Reparixin L-lysine salt (Repertaxin; DF 1681Y) Cat. No.: HY-15251 (Repertaxin L-lysine salt) Cat. No.: HY-15252

Bioactivity: Reparixin is a non-competitive allosteric inhibitor of the Bioactivity: Reparixin L-lysine salt is an allosteric inhibitor of

chemokine receptors CXCR1 and CXCR2 activation with IC50s of chemokine receptor 1/2 (CXCR1/2) activation. 1 and 100 nM, respectively.

Purity: 99.98% Purity: 99.97% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 35

SB225002 SCH 546738 Cat. No.: HY-16711 Cat. No.: HY-10017

Bioactivity: SB225002 is a potent and selective CXCR2 antagonist with an Bioactivity: SCH 546738 is a novel, potent and non-competitive CXCR3

IC50 of 22 nM. antagonist, the affinity constant ( Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.

Purity: 99.58% Purity: 99.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

SCH 563705 SRT3109 Cat. No.: HY-10011 Cat. No.: HY-15462

Bioactivity: SCH 563705 is a potent and orally available CXCR2 and CXCR1 Bioactivity: SRT3109 is an antagonist of CXCR2, with a pIC50 of 8.2, and antagonist, with IC s of 1.3 nM, 7.3 nM and K s of 1 and 3 50 i used in the research of chemokine mediated diseases. nM, respectively.

Purity: 95.34% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg 5 mg

SRT3190 TAK-779 Cat. No.: HY-13021 (Takeda 779) Cat. No.: HY-13406

Bioactivity: SRT3190 is an antagonist of CXCR2, used in the research of Bioactivity: TAK-779 is a potent and selective nonpeptide antagonist of

chemokine mediated diseases. CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and

effectively and selectively inhibits R5 HIV-1, with EC50 …

Purity: 99.61% Purity: 99.73% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg

UNBS5162 USL311 Cat. No.: HY-16509 Cat. No.: HY-114244

Bioactivity: UNBS5162 is a pan-antagonist of CXCL chemokine expression, Bioactivity: USL311 is a selective CXCR4 antagonist, with anti-tumor with anti-tumor activity. activity. USL311 prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4 [1].

Purity: 99.75% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

WZ811 Cat. No.: HY-15478

Bioactivity: WZ811 is a potent CXCR4 antagonist, effectively inhibits

TN14003 binding to CXCR4, with an EC50 of 0.3 nM.

Purity: 99.74% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

36 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] FKBP FK506-binding protein

www.MedChemExpress.com 37 FKBP Inhibitors & Modulators

AP1867 AP20187 Cat. No.: HY-114434 (B/B Homodimerizer) Cat. No.: HY-13992

Bioactivity: AP1867 is a synthetic FKBP12 F36V-directed ligand. Bioactivity: AP20187 (B/B Homodimerizer) is a cell-permeable ligand used to dimerize FK506-binding protein ( FKBP) fusion proteins and initiate biological signaling cascades and gene expression or disrupt protein-protein interactions.

Purity: >98% Purity: 99.80% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

Everolimus PROTAC FKBP12-binding moiety 1 (RAD001; SDZ-RAD) Cat. No.: HY-10218 Cat. No.: HY-107452

Bioactivity: Everolimus (RAD001) is a potent mTOR inhibitor that binds Bioactivity: PROTAC FKBP12-binding moiety 1 is a synthetic ligand for FKBP to FKBP-12 to generate an immunosuppressive complex. (SLF), which is used in the synthesis of PROTACs.

Purity: 98.79% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 500 mg, 250 mg

Rapamycin Rimiducid (Sirolimus; AY 22989) Cat. No.: HY-10219 (AP1903) Cat. No.: HY-16046

Bioactivity: Rapamycin (Sirolimus; AY 22989) is a potent and specific Bioactivity: Rimiducid (AP1903) is a dimerizer agent that acts by

mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. cross-linking the FKBP domains, initiating Fas signaling and Rapamycin binds to FKBP12 and specifically acts as an hence apoptosis. allosteric inhibitor of mTORC1 [1]. Rapamycin is… Purity: 99.93% Purity: 99.81% Clinical Data: Launched Clinical Data: Phase 2 Size: 50 mg, 100 mg, 200 mg, 500 mg, 1 g, 2 g, 5 g Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

SAFit1 SAFit2 Cat. No.: HY-102079 Cat. No.: HY-102080

Bioactivity: SAFit1 is a FK506 binding protein 51 ( FKBP51)-specific Bioactivity: SAFit2 is a novel, selective FK506-binding protein 51 ( [1] [2] FKBP51) antagonist with a K of 6 nM and also enhances inhibitor with a Ki of 4±0.3 nM . i AKT2-AS160 binding.

Purity: >98% Purity: 98.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg

Tacrolimus Tacrolimus monohydrate (FK506 (monohydrate); Fujimycin (FK506; Fujimycin; FR900506) Cat. No.: HY-13756 (monohydrate); FR900506 (monohydrate)) Cat. No.: HY-13756A

Bioactivity: Tacrolimus (FK506; Fujimycin) is a macrocyclic lactone with Bioactivity: Tacrolimus monohydrate (FK506 monohydrate; Fujimycin potent immunosuppressive properties. Tacrolimus binds to monohydrate) binds to FK506 binding protein ( FKBP). This FK506 binding protein (FKBP) to form a complex and inhibits complex inhibits calcineurin phosphatase (PP2B). Tacrolimus calcineurin phosphatase. monohydrate is a mTOR-independent autophagy inducer.

Purity: 98.46% Purity: 98.46% Clinical Data: Launched Clinical Data: Launched Size: 10 mg, 50 mg, 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

38 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] FLAP 5-lipoxygenase-activating protein;5-LO activating protein

FLAP (Arachidonate 5-lipoxygenase-activating protein) is a protein that in humans is encoded by the ALOX5AP gene. FLAP is necessary for the activation of 5-lipoxygenase and therefore for the production of leukotrienes. It is an integral protein within the nuclear membrane. FLAP is necessary in synthesis of leukotriene, which are lipid mediators of inflammation that is involved in respiratory and cardiovascular diseases. FLAP functions as a membrane anchor for 5-lipooxygenase and as an amine acid-bind protein. Gene polymorphisms in FLAP are suspected of playing a role in Alzheimer's disease. Leukotrienes, which need the FLAP protein to be made, have an established pathological role in allergic and respiratory diseases. Animal and human genetic evidence suggests they may also have an important role in atherosclerosis, myocardial infarction, and stroke. The structure of FLAP provides a tool for the development of novel therapies for respiratory and cardiovascular diseases and for the design of focused experiments to probe the cell biology of FLAP and its role in leukotriene biosynthesis.

www.MedChemExpress.com 39 FLAP Inhibitors & Modulators

AM 103 AM679 Cat. No.: HY-14163 Cat. No.: HY-14460

Bioactivity: AM 103 is a potent and selective FLAP inhibitor, with an IC50 Bioactivity: AM679 is a potent and selective FLAP inhibitor with IC50s of value of 4.2 nM. 2.2 nM/0.6 nM/154 nM for FLAP binding/hLA/hWB respectively.

Purity: >98% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

Fiboflapon Fiboflapon sodium (GSK2190915; AM-803) Cat. No.: HY-15874 (GSK2190915 (sodium salt); AM-803 sodium) Cat. No.: HY-15874A

Bioactivity: Fiboflapon (GSK2190915) is a potent Bioactivity: Fiboflapon sodium (GSK2190915 (sodium salt)) is a potent FLAP(5-Lipoxygenase-activating protein) inhibitor with binding FLAP(5-Lipoxygenase-activating protein) inhibitor with binding

IC 50 of 2.9 nM. IC 50 of 2.9 nM.

Purity: 98.18% Purity: 99.08% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

MK-886 MK591 free acid (L 663536) Cat. No.: HY-14166 (Quiflapon) Cat. No.: HY-10037

Bioactivity: MK886 is a 5-lipoxygenase-activating protein inhibitor and a Bioactivity: MK591 (free acid) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC leukotriene biosynthesis inhibitor ( IC50=2.5 nM). 50 value of 1.6 nM in a FLAP binding assay.

Purity: 99.77% Purity: 99.44% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Quiflapon sodium (MK591) Cat. No.: HY-50714

Bioactivity: Quiflapon sodium (MK591) is a selective and specific 5-Lipoxygenase-activating protein ( FLAP) inhibitor.

Purity: 99.25% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

40 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Galectin

Galectins are a family of proteins that possess β-galactoside-binding properties through their carbohydrate recognition domains (CRDs). Galectins can be secreted from cells by nonclassic pathways to interact with external glycoconjugates and have a variety of activities both extra- and intracellularly, with important implicated roles in immunity, inflammation, and cancer. Galectins can be classified according to the CRD features. Galectin-1, -2, -5, -7, -10, -11, -13, and -14 are composed of a CRD and a short N-terminal sequence (prototype). Galectin-4, -6, -8, -9, and -12 have two nonidentical CRDs in tandem with a short linker sequence (tandem-repeat type). Galectin-3 has an exceptional structure, with a CRD and an extended N-terminal domainconsisting of gycine/proline-rich repeats and a short N-terminal end (chimera type). Galectin-1 (Gal1), a carbohydrate-binding protein is implicated in cancer cell proliferation, invasion and tumour angiogenesis. Galectin-3 (Gal3) is a β-galactoside binding lectin that is highly expressed in fibrotic tissue of diverse etiologies. Galectins have emerged as key players in the tumor microenvironment. Galectins are expressed and released by different celltypes, including tumor, stromal, endothelial and immune cells. Galectins critically influence tumor progression by modulating tumor cell migration, invasiveness, angiogenesis and antitumor immune responses. Intracellularly, galectins modulate survival and proliferation and they interact with a variety of signaling pathways. Given these extracellular and intracellular functions and their regulated expression at sites of tumor growth and metastasis, galectins have stimulated great interest as relevant biomarkers and novel targets in cancer therapy.

www.MedChemExpress.com 41 Galectin Inhibitors & Modulators

G3-C12 G3-C12 TFA Cat. No.: HY-P1592 Cat. No.: HY-P1592A

Bioactivity: G3-C12 is a galectin-3 binding peptide, with Kd of 88 nM, Bioactivity: G3-C12 (TFA) is a galectin-3 binding peptide, with Kd of 88 and shows anticancer activity. nM, and shows anticancer activity.

Purity: >98% Purity: 99.44% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 1 mg, 5 mg, 10 mg

OTX008 TD139 (Calixarene 0118; PTX008) Cat. No.: HY-19756 Cat. No.: HY-19940

Bioactivity: OTX008 is a selective inhibitor of galectin-1. Bioactivity: TD139 is an inhaled galectin-3 inhibitor with a Kd of 14 nM.

Purity: 99.36% Purity: 99.39% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

42 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Histamine Receptor

Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

www.MedChemExpress.com 43 Histamine Receptor Inhibitors & Modulators

(±)-Methotrimeprazine (D6) (±)-Tazifylline (dl-Methotrimeprazine D6) Cat. No.: HY-19489S Cat. No.: HY-U00018

Bioactivity: (±)-Methotrimeprazine (D6) is the deuterium labeled Bioactivity: (±)-Tazifylline is a potent, selective and long-acting Methotrimeprazine, which is a D3 dopamine and Histamine H1 histamine H1 receptor antagonist. receptor antagonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

ABT-239 Acrivastine Cat. No.: HY-12195 (BW825C) Cat. No.: HY-B1510

Bioactivity: ABT-239 is a novel, highly efficacious, Bioactivity: Acrivastine (BW825C) is a short acting histamine 1 non-imidazole class of H3R antagonist and a transient receptor antagonist for the treatment of allergic rhinitis. receptor potential vanilloid type 1 ( TRPV1) antagonist.

Purity: 98.94% Purity: 98.00% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 10 mg, 50 mg, 100 mg

Alcaftadine Alimemazine D6 (R89674) Cat. No.: HY-17039 (Trimeprazine D6) Cat. No.: HY-12752S

Bioactivity: Alcaftadine(R89674) is a H1 histamine receptor antagonist, Bioactivity: Alimemazine D6 is deuterium labeled Alimemazine, which is an which is used to prevent eye irritation brought on by allergic antihistamine. conjunctivitis.

Purity: 97.17% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 50 mg, 100 mg

Antazoline hydrochloride Antihistamine-1 (Phenazoline hydrochloride) Cat. No.: HY-B1067 Cat. No.: HY-100238

Bioactivity: Antazoline hydrochloride is a 1st generation antihistamine Bioactivity: Antihistamine-1 is a H1-antihistamine ( Ki=6.9 nM) with with also anticholinergic properties used to relieve nasal acceptable blood-brain barrier penetration and also an congestion and in eye drops. inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively. Purity: 99.36% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 100 mg

Astemizole Azatadine (R 43512) Cat. No.: HY-12532 Cat. No.: HY-B0170

Bioactivity: Astemizole, a second-generation antihistamine drug to diminish Bioactivity: Azatadine is an histamine and cholinergic inhibitor with IC50 allergic symptoms with a long duration of action, is a of 6.5 nM and 10 nM, respectively. Target: Histamine Receptor

histamine H1-receptor antagonist, with an IC50 of 4 nM. Azatadine, a new antihistamine, was evaluated for its efficacy Astemizole also shows potent hERG K+ channel blocking activ… in 20 patients with chronic allergic rhinitis. Eighty percent of patients had symptomatic relief with a twice daily dosage… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: Size: 10 mg, 50 mg, 100 mg

44 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Azatadine dimaleate Azelastine (Azatadine maleate) Cat. No.: HY-B0170A Cat. No.: HY-B0462A

Bioactivity: Azatadine dimaleate is an histamine and cholinergic inhibitor Bioactivity: Azelastine is a potent, second-generation, selective, with IC50 of 6.5 nM and 10 nM, respectively. Target: Histamine histamine antagonist. Receptor Azatadine, a new antihistamine, was evaluated for its efficacy in 20 patients with chronic allergic rhinitis. Eighty percent of patients had symptomatic relief with a twice daily… Purity: 99.85% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg 10 mg, 50 mg, 100 mg

Azelastine hydrochloride Bamirastine Cat. No.: HY-B0462 (TAK-427) Cat. No.: HY-101601

Bioactivity: Azelastine HCl is a potent, second-generation, selective, Bioactivity: Bamirastine inhibits ligand binding to recombinant human

histamine antagonist. histamine H 1 receptors ( rhH1R) with an IC50 value of 17.3 nM.

Purity: 99.95% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg, 200 mg

Bavisant Bavisant dihydrochloride (JNJ-31001074) Cat. No.: HY-14880 Cat. No.: HY-14880A

Bioactivity: Bavisant (JNJ-31001074) is a highly selective, orally active Bioactivity: Bavisant Hcl (JNJ-31001074) is a highly selective, orally antagonist of the human H3 receptor with a novel mechanism of active antagonist of the human H3 receptor with a novel action, involving wakefulness and cognition, with potential as mechanism of action, involving wakefulness and cognition, with a treatment for ADHD. potential as a treatment for ADHD.

Purity: >98% Purity: >98% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

Bavisant dihydrochloride hydrate Bepotastine Beslilate (JNJ31001074AAC) Cat. No.: HY-14880B Cat. No.: HY-A0015

Bioactivity: Bavisant Hcl hydrate(JNJ-31001074) is a highly selective, Bioactivity: Bepotastine Beslilate (Bepreve) is a histamine H1 receptor orally active antagonist of the human H3 receptor with a novel anatagonist. mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

Purity: 99.77% Purity: 99.36% Clinical Data: Phase 2 Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Betahistine dihydrochloride Bilastine Cat. No.: HY-B0524A Cat. No.: HY-14447

Bioactivity: Betahistine Dihydrochloride is a histamine H3 receptors Bioactivity: Bilastine is a selective histamine H1 receptor antagonist used inhibitor used as an antivertigo drug. for treatment of allergic rhinoconjunctivitis and urticaria.

Purity: 99.88% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 g, 5 g, 10 g 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 45

BMY-25271 Brompheniramine maleate Cat. No.: HY-100191 Cat. No.: HY-B0480

Bioactivity: BMY-25271 is a histamine H2 receptor antagonist. Bioactivity: Brompheniramine maleate is a histamine H1 receptors antagonist.

Purity: >98% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg

Carbinoxamine maleate salt Cetirizine Cat. No.: HY-B1589A Cat. No.: HY-17042

Bioactivity: Carbinoxamine maleate salt is a histamine H1 receptor Bioactivity: Cetirizine, a second-generation antihistamine, is a major antagonist. metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value: Target: Histamine H1 receptor Cetirizine crosses the blood-brain barrier only… Purity: 99.78% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 100 mg, 200 mg, 500 mg 100 mg, 500 mg

Cetirizine D4 dihydrochloride Cetirizine D8 dihydrochloride Cat. No.: HY-17042AS Cat. No.: HY-17042AS1

Bioactivity: Cetirizine D4 2Hcl is deuterium labeled Cetirizine, which is a Bioactivity: Cetirizine D8 2Hcl is deuterium labeled Cetirizine, which is a major metabolite of hydroxyzine, and a racemic selective H1 major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist. receptor inverse agonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

Cetirizine dihydrochloride Chlorcyclizine hydrochloride (P071) Cat. No.: HY-17042A Cat. No.: HY-112067A

Bioactivity: Cetirizine 2Hcl, a second-generation antihistamine, is a major Bioactivity: Chlorcyclizine hydrochloride is a histamine H1 antagonist. metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. IC50 value: Target: Histamine H1 receptor Cetirizine crosses the blood-brain barrier only… Purity: 99.17% Purity: 99.90% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg 100 mg, 200 mg, 500 mg

Chloropyramine hydrochloride Chlorpheniramine maleate Cat. No.: HY-B1305 (Chlorphenamine maleate) Cat. No.: HY-B0286A

Bioactivity: Chloropyramine hydrochloride is a histamine receptor H1 Bioactivity: Chlorpheniramine maleate is an histamine H1 receptor antagonist which can also inhibit the biochemical function of antagonist with IC50 of 12 nM. VEGFR-3 and FAK.

Purity: 99.30% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 1 g, 5 g

46 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Chlorphenoxamine CI-949 Cat. No.: HY-B1607 Cat. No.: HY-U00364

Bioactivity: Chlorphenoxamine is an antihistamine and anticholinergic used Bioactivity: CI-949 is an allergic mediator release inhibitor, which

as an antipruritic and antiparkinsonian agent. inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and

thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively. Purity: 95.09% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 50 mg

Cimetidine Cinnarizine (SKF-92334) Cat. No.: HY-14289 Cat. No.: HY-B1090

Bioactivity: Cimetidine is a histamine-2 (H2) receptor antagonist. Bioactivity: Cinnarizine is an antihistamine and a calcium channel blocker, promote cerebral blood flow, used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis.

Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 1 g, 5 g, 10 g Size: 10mM x 1mL in DMSO, 100 mg

Cipralisant Ciproxifan (GT-2331) Cat. No.: HY-106993 (FUB-359) Cat. No.: HY-14567

Bioactivity: Cipralisant is a potent and selective histamine H3 Bioactivity: Ciproxifan(FUB-359) is a highly potent and selective histamin receptor antagonist in vivo, and an agonist in vitro, with a H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity… Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 5 mg, 10 mg, 50 mg

Ciproxifan maleate Clemastine fumarate (FUB 359 maleate) Cat. No.: HY-15289 (HS-592 (fumarate); Meclastine (fumarate)) Cat. No.: HY-B0298A

Bioactivity: Ciproxifan maleate(FUB-359 maleate) is a highly potent and Bioactivity: Clemastine (fumarate) (HS-592 (fumarate)) is a selective

selective histamin H3-receptor antagonist with IC50 of 9.2 nM, histamine H1 receptor antagonist with IC 50 of 3 nM. with low apparent affinity at other receptor subtypes.

Purity: 99.56% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 100 mg, 200 mg, 500 mg

Clemizole Clemizole hydrochloride Cat. No.: HY-30234 Cat. No.: HY-30234A

Bioactivity: Clemizole is an H1 histamine receptor antagonist, is found Bioactivity: Clemizole hydrochloride is an H1 histamine receptor

to substantially inhibit HCV replication. The IC50 of antagonist, is found to substantially inhibit HCV replication. The IC of Clemizole for RNA binding by NS4B is Clemizole for RNA binding by NS4B is 24±1 nM, whereas its 50

EC50 for viral replication is 8 µM. 24±1 nM, whereas its EC50 for viral replication is 8 µM. Purity: >98% Purity: 99.32% Clinical Data: Launched Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 47

CP-66948 Cyproheptadine hydrochloride sesquihydrate Cat. No.: HY-19048 Cat. No.: HY-B1165

Bioactivity: CP-66948 is a histamine H2-receptor antagonist with Bioactivity: Cyproheptadine hydrochloride sesquihydrate is an antihistamine gastric antisecretory activity and mucosal protective and is an antagonist of serotonin and histamine2. properties.

Purity: >98% Purity: 99.20% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 100 mg

Decloxizine Decloxizine dihydrochloride (UCB-1402; NSC289116) Cat. No.: HY-17582 (UCB 1402 dihydrochloride) Cat. No.: HY-A0075

Bioactivity: Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor Bioactivity: Decloxizine dihydrochloride(UCB-1402; NSC289116) is a antagonist. histamine 1 receptor antagonist.

Purity: >98% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 50 mg, 100 mg, 500 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg

Desloratadine Dexchlorpheniramine maleate (Sch34117) Cat. No.: HY-B0539 (S-(+)-Chlorpheniramine maleate salt) Cat. No.: HY-B1062

Bioactivity: Desloratadine(Sch34117) is a potent antagonist for human Bioactivity: Dexchlorpheniramine maleate is an antihistamine, with histamine H1 receptor used to treat allergies. anticholinergic properties, used to treat allergic conditions.

Purity: 99.75% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 500 mg 200 mg

Dimenhydrinate Diphenhydramine hydrochloride Cat. No.: HY-B1215 Cat. No.: HY-B0303A

Bioactivity: Dimenhydrinate is an anti-emetic and anti-histamine commonly Bioactivity: Diphenhydramine HCl (Benadryl), a histamine H1 antagonist used available over-the-counter as a motion sickness remedy. as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. Target: Histamine H1 receptor Diphenhydramine… Purity: 99.89% Purity: 99.75% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 250 mg, 500 mg, 5 g

Diphenylpyraline hydrochloride Doxylamine D5 succinate (4-Diphenylmethoxy-1-methylpiperidine hydrochloride) Cat. No.: HY-B0970 Cat. No.: HY-A0069S

Bioactivity: Diphenylpyraline Hcl is a first-generation antihistamine with Bioactivity: Doxylamine D5 succinate is deuterium labeled Doxylamine, which anticholinergic effects, acts as a dopamine reuptake is a first generation antihistamine. inhibitor, shows to be useful in the treatment of Parkinsonism.

Purity: 99.02% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg 1 g

48 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Doxylamine succinate Ebastine Cat. No.: HY-A0069 (LAS-W 090; RP64305) Cat. No.: HY-B0674

Bioactivity: Doxylamine (succinate) is a first generation antihistamine; Bioactivity: Ebastine(LAS-W 090;RP64305) is a long-acting and selective can be used by itself as a short-term sedative and in H1-histamine receptor antagonist. Target: Histamine H1 combination with other drugs to provide night-time allergy and Receptor Ebastine is a H1 antihistamine with low potential for cold relief. causing drowsiness. Ebastine (10 mg orally) causes brain histamine H1-receptor occupation of approximately 10%,… Purity: 99.77% Purity: 99.96% Clinical Data: Launched Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Ethanol, 100 mg 500 mg, 1 g, 5 g

Ebrotidine Epinastine (FI3542) Cat. No.: HY-15538 (WAL801) Cat. No.: HY-B0640

Bioactivity: Ebrotidine(FI 3542) is a competitive H2-receptor antagonist Bioactivity: Epinastine(WAL801) is an antihistamine and mast cell (Ki= 127.5 nM) with a potent antisecretory activity and stabilizer that is used in eye drops to treat allergic evidenced gastroprotection. conjunctivitis.

Purity: 97.78% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 50 mg, 100 mg, 500 mg

Famotidine Fenspiride Hydrochloride (MK-208) Cat. No.: HY-B0377 Cat. No.: HY-A0027

Bioactivity: Famotidine (MK-208) is a competitive histamine H2-receptor Bioactivity: Fenspiride Hcl is an α adrenergic and H1 histamine receptor antagonist. Its main pharmacodynamic effect is the inhibition antagonist. of gastric secretion.

Purity: 98.17% Purity: 99.03% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg

Fexofenadine D6 Fexofenadine hydrochloride (MDL-16455 hydrochloride; (MDL-16455 D6) Cat. No.: HY-B0801S Terfenidine carboxylate hydrochloride) Cat. No.: HY-B0801A

Bioactivity: Fexofenadine D6 is deuterium labeled is Fexofenadine, which is Bioactivity: Fexofenadine hydrochloride (MDL-16455 hydrochloride; an antihistamine pharmaceutical drug. Terfenidine carboxylate hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years) [1].

Purity: 98.0% Purity: 99.61% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

FRG8701 GSK189254A Cat. No.: HY-U00238 Cat. No.: HY-14111

Bioactivity: FRG-8701 is a new Histamine H2-receptor antagonist with Bioactivity: GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 an IC50 of ranging from 0.25 to 0.43 μM. and 8.51-9.17 for human and rat H3, respectively.

Purity: >98% Purity: 98.58% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 49

H3 receptor antagonist 1 H3 receptor-MO-1 Cat. No.: HY-U00269 Cat. No.: HY-U00339

Bioactivity: H3 receptor antagonist 1 is an antagonist of histamine H3 Bioactivity: H3 receptor-MO-1 is a modulator of histamine H3 receptor. receptor, used in the research of neurological disease.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 1 mg, 5 mg, 10 mg, 20 mg

H3R-IN-1 Hydrochloride H4 Receptor antagonist 1 Cat. No.: HY-112219A Cat. No.: HY-114025

Bioactivity: H3R-IN-1 Hydrochloride is a histamine receptor 3 ( H3R) Bioactivity: H4 Receptor antagonist 1 is a potent and selective

inverse agonist extracted from patent WO2013107336A1, compound histamine H4 receptor inverse agonist, with an IC50 of 19 example 2. nM.

Purity: 95.52% Purity: 99.70% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

H4R antagonist 1 Histamine Cat. No.: HY-111501 (Ergamine) Cat. No.: HY-B1204

Bioactivity: H4R antagonist 1 is a potent and highly selective histamine Bioactivity: Histamine is an organic nitrogenous compound involved in local

H4 receptor ( H4R) antagonist with an IC 50 of 27 nM. H4R immune responses as well as regulating physiological function antagonist 1 does not show any noticeable binding affinity… in the gut and acting as a neurotransmitter.

Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in Water, 100 mg

Histamine phosphate Hydroxyzine (Histamine diphosphate) Cat. No.: HY-A0129 Cat. No.: HY-B0548

Bioactivity: Histamine diphosphate is a potent agonist of histamine Bioactivity: Hydroxyzine is a histamine H1-receptor antagonist. receptors and vasodilator. It can activate nitric oxide synthetase.

Purity: 99.79% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 100 mg, 500 mg 1 g

Hydroxyzine D4 dihydrochloride Hydroxyzine dihydrochloride Cat. No.: HY-B0548AS Cat. No.: HY-B0548A

Bioactivity: Hydroxyzine D4 2Hcl is deuterium labeled Hydroxyzine, which is Bioactivity: Hydroxyzine Dihydrochloride is a histamine H1-receptor a histamine H1-receptor antagonist. antagonist. Target: Histamine H1-Receptor Hydroxyzine inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the… Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10mM x 1mL in Water, 100 mg, 500 mg

50 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Hydroxyzine pamoate JNJ-39758979 Cat. No.: HY-B0895 Cat. No.: HY-101189

Bioactivity: Hydroxyzine pamoate is a histamine H1-receptor antagonist. Bioactivity: JNJ-39758979 is a selective, high-affinity histamine H4 Target: Histamine H1-Receptor Hydroxyzine inhibits carbachol receptor antagonist with a K of 12.5 nM. (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM i and by 17% 0.1 μM in pretreated bladder slices for 60 min [1]. Hydroxyzine (0.1 mM) treatment inhibits the progression and… Purity: >98% Purity: 98.01% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

JNJ-5207852 JNJ-7777120 Cat. No.: HY-12190 Cat. No.: HY-13508

Bioactivity: JNJ-5207852 is a selective and potent histamine H3 Bioactivity: JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, receptor (H R) antagonist, with pK s of 8.9, 9.24 for rat exhibits >1000-fold selectivity over the other histamin 3 i receptors. and human H 3R, respectively.

Purity: 98.0% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

Ketotifen fumarate KP136 (HC 20511 fumarate) Cat. No.: HY-B0157A (AL136) Cat. No.: HY-U00168

Bioactivity: Ketotifen (fumarate) is a second-generation noncompetitive Bioactivity: KP136 is an orally effective antiallergic agent. The IC50 is H1-antihistamine and mast cell stabilizer, which is used to 76.1 μg/mL for histamine release and 63 ug/mL for prevent asthma attacks. degranulation.

Purity: 99.92% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 200 mg, 1 g

Lafutidine Latrepirdine dihydrochloride (FRG-8813) Cat. No.: HY-B0160 (Dimebolin dihydrochloride) Cat. No.: HY-14537

Bioactivity: Lafutidine, a newly developed histamine H(2)-receptor Bioactivity: Latrepirdine dihydrochloride is a neuroactive compound with antagonist, inhibits gastric acid secretion. antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β ( Aβ) secretion. Purity: 97.86% Purity: 99.75% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

Levodropropizine Lodoxamide (DF-526; (S)-(-)-Dropropizine) Cat. No.: HY-B1895 Cat. No.: HY-14270

Bioactivity: Levodropropizine (DF-526) is a histamine receptor inhibitor, Bioactivity: Lodoxamide is an antiallergic compound acting as a mast-cell Levodropropizine is an effective and very well tolerated stabilizer for the treatment of asthma and allergic peripheral antitussive drug. conjunctivitis.

Purity: 99.92% Purity: 98.00% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

www.MedChemExpress.com 51

Lodoxamide tromethamine Loratadine (U 42585 E) Cat. No.: HY-16289 (SCH 29851; Loratidine) Cat. No.: HY-17043

Bioactivity: Lodoxamide tromethamine (U 42585 E) is a medication for the Bioactivity: Loratadine(SCH-29851) is a selective inverse peripheral treatment of prophylaxis of mast cell-mediated allergic histamine H1-receptor agonist with an IC50 of >32 μM. IC50 disease. value: 32 uM Target: H1-receptor Loratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells. Purity: 98.0% Purity: 99.95% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 10 mg, 50 mg, 100 mg

Mebhydrolin Mebhydrolin napadisylate Cat. No.: HY-B1303A (Mebhydroline 1,5-naphthalenedisulfonate salt) Cat. No.: HY-B1303

Bioactivity: Mebhydrolin is a specific histamine H1 receptor Bioactivity: Mebhydrolin napadisylate is a specific histamine H1 antagonist. receptor antagonist.

Purity: 99.46% Purity: 99.53% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg

Meclizine dihydrochloride Mepyramine maleate (Meclozine dihydrochloride; NSC28728) Cat. No.: HY-B0349 (Pyrilamine maleate) Cat. No.: HY-B1281

Bioactivity: Meclizine is a histamine H1 receptor antagonist used to treat Bioactivity: Mepyramine maleate, a first generation antihistamine, is an

nausea and motion sickness Target: Histamine H1 Receptor antagonist of histamine H1 receptor, with Kds of 0.8 nM, Meclizine is a histamine H1 receptor antagonist used to treat 5200 nM and >3000 nM for H1, H2, and H3 receptor, nausea and motion sickness, possesses anticholinergic, central respectively, and a pK of 9.4 for H1 receptor. nervous system depressant, and local anesthetic effects [1].… d Purity: 99.97% Purity: 99.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 5 g 100 mg

Mequitazine Metiamide (LM-209) Cat. No.: HY-B2168 (SK&F 92058) Cat. No.: HY-15540

Bioactivity: Mequitazine is a potent, nonsedative and long-acting histamine Bioactivity: Metiamide (SK&F 92058) is a histamine H2-receptor

H1 antagonist. antagonist developed from another H2 antagonist, burimamide.

Purity: 99.93% Purity: 97.31% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg

Mianserin Mianserin hydrochloride (Mianserine) Cat. No.: HY-B0188 (Org GB 94) Cat. No.: HY-B0188A

Bioactivity: Mianserin is a H1 receptor inverse agonist and is a Bioactivity: Mianserin hydrochloride is a H1 receptor inverse agonist and psychoactive agent of the tetracyclic antidepressant. is a psychoactive agent of the tetracyclic antidepressant. Target: H1 receptor Mianserin is a psychoactive drug of the tetracyclic antidepressant (TeCA) therapeutic family. It is classified as a noradrenergic and specific serotonergic… Purity: >98% Purity: 99.79% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg

52 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Mizolastine Mizolastine dihydrochloride Cat. No.: HY-B0164 Cat. No.: HY-B0164A

Bioactivity: Mizolastine is a histamine H1-receptor antagonist with IC50 of Bioactivity: Mizolastine dihydrochloride is a histamine H1-receptor 47 nM used in the treatment of hay fever (seasonal allergic antagonist with IC50 of 47 nM used in the treatment of hay rhinitis), hives and other allergic reactions. fever (seasonal allergic rhinitis), hives and other allergic reactions.

Purity: 99.33% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 200 mg, 500 mg Size: 100 mg, 200 mg, 500 mg

MK-0249 N-Acetylhistamine Cat. No.: HY-U00076 (N-Omega-acetylhistamine) Cat. No.: HY-112175

Bioactivity: MK-0249 is a potent histamine H3 receptor antagonist, with Bioactivity: N-Acetylhistamine is a histamine metabolite. N-acetylhistamine can be used as a potential biomarker of histidine metabolism Ki of 1.7 nM for human H3. for anaphylactoid reactions.

Purity: >98% Purity: 98.99% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 50 mg

Nedocromil Nedocromil sodium (FPL 59002) Cat. No.: HY-13448 (FPL 59002KP; Nedocromil disodium salt) Cat. No.: HY-16344

Bioactivity: Nedocromil suppresses the action or formation of multiple Bioactivity: Nedocromil sodium suppresses the action or formation of

mediators, including histamine, leukotriene C4 ( LTC4), multiple mediators, including histamine, leukotriene C4 (

and prostaglandin D2 ( PGD2). LTC4), and prostaglandin D2 ( PGD2).

Purity: 95.66% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 5 mg, 10 mg

Niperotidine Nizatidine Cat. No.: HY-15539 Cat. No.: HY-B0310

Bioactivity: Niperotidine is a histamine H2-receptor antagonist. Bioactivity: Nizatidine is a histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion.

Purity: >98% Purity: 99.49% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 1 g, 5 g

Olopatadine hydrochloride Osthole (ALO4943A; KW4679) Cat. No.: HY-B0426A (NSC 31868; Osthol; Ostol) Cat. No.: HY-N0054

Bioactivity: Olopatadine HCl is a histamine blocker used to treat allergic Bioactivity: Osthole is a natural antihistamine alternative. Osthole may be

conjunctivitis. a potential inhibitor of histamine H1 receptor activity.

Purity: 99.55% Purity: 99.90% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 250 mg, 1 g, 5 g

www.MedChemExpress.com 53

Pemirolast potassium Peptide 401 (TWT-8152; BMY 26517) Cat. No.: HY-B0538A Cat. No.: HY-12537

Bioactivity: Pemirolast Potassium (BMY 26517) is a histamine H1 antagonist Bioactivity: Peptide 401, a potent mast cell degranulating factor from bee and mast cell stabilizer that acts as an antiallergic agent. venom, suppresses the increased vascular permeability due to Target: Histamine H1 Receptor Pemirolast potassium (BMY 26517) intradermal injection of various smooth muscle spasmogens ( is a new oral, nonbronchodilator antiallergy medication that histamine, and 5-HT). is being evaluated for the therapy of asthma [1]. Pemirolast… Purity: 99.96% Purity: 98.29% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 500u g, 1 mg, 5 mg 10 mg, 50 mg, 100 mg

Perphenazine Perphenazine D8 Dihydrochloride Cat. No.: HY-A0077 Cat. No.: HY-A0077AS

Bioactivity: Perphenazine is a typical antipsychotic drug, inhibits Bioactivity: Perphenazine D8 Dihydrochloride is the deuterium labeled

5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine Perphenazine, which is a typical antipsychotic drug(5-HT, receptor D2/D3, D2L receptor, and Histamine H1 receptor, Dopamine receptor ligand).

with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 … Purity: 99.90% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg 1 g, 5 g

PF-3893787 hydrochloride Pheniramine Maleate Cat. No.: HY-19705B Cat. No.: HY-B0971

Bioactivity: PF-3893787 hydrochloride is a novel histamine H4 receptor Bioactivity: Pheniramine Maleate ia an antihistamine and vasoconstrictor.

antagonist binding affinity ( Ki=2.4 nM) and is also a

functional ( Ki=1.56 nM) antagonist.

Purity: 98.0% Purity: 99.88% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg, 500 mg

Pimethixene Pimethixene maleate (Pimetixene) Cat. No.: HY-B1101 (Pimetixene maleate) Cat. No.: HY-B1101A

Bioactivity: Pimethixene is antihistamine and antiserotonergic compound, Bioactivity: Pimethixene maleate is antihistamine and antiserotonergic acts as an antimigraine agent. Pimethixene is a highly potent compound, acts as an antimigraine agent. Pimethixene maleate

antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B, 5-HT 2C, is a highly potent antagonist of 5-HT 1A, 5-HT 2A, 5-HT 2B,

histamine H 1, dopamine D 2 and D 4.4 as well as muscari… 5-HT 2C, histamine H 1, dopamine D 2 and D 4.4 as well… Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mg Size: 10 mg

Pirolate Pitolisant (CP-32387) Cat. No.: HY-100280 (Tiprolisant) Cat. No.: HY-12199

Bioactivity: Pirolate is a histamine H1 receptor. Bioactivity: Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (

Ki=0.16 nM).

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10 mg, 50 mg

54 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pitolisant hydrochloride Pitolisant oxalate (Ciproxidine; BF 2649) Cat. No.: HY-12199B (Tiprolisant oxalate) Cat. No.: HY-12199A

Bioactivity: Pitolisant hydrochloride is a potent and selective Bioactivity: Pitolisant oxalate is a potent and selective nonimidazole nonimidazole inverse agonist at the recombinant human inverse agonist at the recombinant human histamine H3

histamine H3 receptor ( Ki=0.16 nM). receptor ( Ki=0.16 nM).

Purity: 99.22% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 10 mg, 50 mg

Promethazine hydrochloride Quinotolast sodium Cat. No.: HY-B0781 (FR71021) Cat. No.: HY-U00027

Bioactivity: Promethazine Hcl(NSC-231688) is the first-generation Bioactivity: Quinotolast sodium in the concentration range of 1-100 μg/mL

antihistamine; strong antagonist of the H1 receptor and inhibits histamine, LTC4 and PGD2 release in a moderate mACh receptor antagonist, moderate affinity for concentration-dependent manner. 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

Purity: 99.82% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 g, 5 g Size: 1 mg, 5 mg, 10 mg, 20 mg

Ranitidine hydrochloride ReN-1869 hydrochloride Cat. No.: HY-B0281A (NNC-05-1869 hydrochloride) Cat. No.: HY-101724

Bioactivity: Ranitidine is a histamine H2-receptor antagonist that inhibits Bioactivity: ReN 1869 hydrochloride is a novel, selective histamine H1 stomach acid production. receptor antagonist, which demonstrates affinity to the

histamine H 1 receptor (guinea pig brain) with K i of 0.19±0.04 μM and the non-selective σ site (guinea pig bra… Purity: 99.48% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 100 mg, 500 mg

Rocastine Roxatidine Acetate Hydrochloride (AHR-11325) Cat. No.: HY-101745 (HOE 760) Cat. No.: HY-B0305A

Bioactivity: Rocastine is a selective, nonsedating H1 antagonist, acting Bioactivity: Roxatidine Acetate HCl is a specific and competitive histamin as an antihistamine. H2 receptor antagonist.

Purity: >98% Purity: 98.87% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in Water, 1 g, 5 g

S 38093 SUN 1334H Cat. No.: HY-104003 Cat. No.: HY-U00084

Bioactivity: S 38093 is a brain-penetrant antagonist of H3 receptor, with Bioactivity: SUN 1334H is a potent, orally active, highly selective H1

Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptor antagonist, with Ki of 9.7 nM. receptors, respectively.

Purity: 99.02% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 55

Toreforant Tripelennamine hydrochloride (JNJ-38518168) Cat. No.: HY-16756 Cat. No.: HY-17428

Bioactivity: Toreforant is a potent and selective histamine H 4 receptor ( Bioactivity: Tripelennamine Hcl, a H1-receptor antagonist, is a H4R) antagonist, with a K at the human receptor of 8.4 nM. psychoactive drug and member of the pyridine i andethylenediamine classes that is used as an antipruritic and first-generation antihistamine. IC50 Value: Target: Histamine H1 receptor Tripelennamine can be used in the treatment of… Purity: >98% Purity: 99.87% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg, 1 g, 5 g

VUF10460 Wy 49051 Cat. No.: HY-101420 Cat. No.: HY-101830

Bioactivity: VUF10460 is a non-imidazole histamine H4 receptor agonist; Bioactivity: Wy 49051 is a potent, orally active H1 receptor antagonist,

binds to rat H4 receptor with a pKi of 7.46. with IC50 of 44 nM.

Purity: 98.37% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Zaltidine (CP-57361) Cat. No.: HY-15541

Bioactivity: Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action.

Purity: 99.0% Clinical Data: No Development Reported Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg

56 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] IFNAR Interferon-α/β receptor;Interferon-alpha/beta receptor

The interferon-α/β receptor (IFNAR) is a receptor which binds type I interferons including interferon-α and -β. It is a heteromeric cell surface receptor composed of one chain with two subunits referred to as IFNAR1 and IFNAR2. Upon binding of type I IFNs, IFNAR activates the JAK-STAT signaling pathway. Interferon stimulation classically results in an anti-viral immune response. Type I IFNs share a common receptor consisting of two subunits, IFNAR1 and IFNAR2, which associate upon IFN binding. IFNAR2 is the major ligand binding component of the receptor complex, exhibiting nanomolar affinity to both IFNα and IFNβ subtypes. IFNAR1 and IFNAR2 belong to the class II helical cytokine receptor (hCR) family, which includes the receptor for type II IFN, tissue factor (TF), and IL10Rβ.

www.MedChemExpress.com 57 IFNAR Inhibitors & Modulators

AX-024 AX-024 hydrochloride Cat. No.: HY-107390 Cat. No.: HY-107390A

Bioactivity: AX-024 is an cytokine release inhibitor which can strongly Bioactivity: AX-024 hydrochloride is an cytokine release inhibitor which can inhibit the production of interleukin-6 ( IL-6), tumor strongly inhibit the production of interleukin-6 ( IL-6), necrosis factor-α ( TNFα), interferon-γ ( IFN-γ), IL-10 and tumor necrosis factor-α ( TNFα), interferon-γ ( IFN-γ), IL-17A. IL-10 and IL-17A.

Purity: 98.0% Purity: 99.29% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CCCP (Carbonyl cyanide 3-chlorophenylhydrazone; Carbonyl IFN alpha-IFNAR-IN-1 Cyanide m-Chlorophenylhydrazone) Cat. No.: HY-100941 Cat. No.: HY-12836

Bioactivity: CCCP is an oxidative phosphorylation uncoupler. Bioactivity: IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM). IC50 value: Target: IFN alpha-IFNAR interaction inhibitor IFN alpha-IFNAR-IN-1 specifically inhibits MVA-induced IFN-α… Purity: 99.83% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg 50 mg

IFN alpha-IFNAR-IN-1 hydrochloride IFN-α Receptor Recognition Peptide 1 Cat. No.: HY-12836A (IRRP1) Cat. No.: HY-P1758

Bioactivity: IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, Bioactivity: IFN-α Receptor Recognition Peptide 1 is a peptide of IFN-α low-molecular-weight inhibitor of the interaction between associated with receptor interactions [1]. IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM). IC50 value: Target: IFN alpha-IFNAR interaction inhibitor IFN alpha-IFNAR-IN-1 specifically… Purity: 99.76% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg, 100 mg

Interferon receptor inducer-1 Cat. No.: HY-112189

Bioactivity: Interferon receptor inducer-1 (compound 6) is an interferon (IFN) receptor inducer. Used accordingly in the treatment of a disorder in which the induction of interferon is involved [1].

Purity: 98.49% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

58 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Interleukin Related IL

Interleukins are a group of cytokines (secreted proteins and signaling molecules) that were first seen to be expressed by white blood cells (leukocytes). The function of the immune system depends in a large part on interleukins, and rare deficiencies of a number of them have been described, all featuring autoimmune diseases or immune deficiency. The majority of interleukins are synthesized by helper CD4 T lymphocytes, as well as through monocytes, macrophages, and endothelial cells. They promote the development and differentiation of T and B lymphocytes, and hematopoietic cells. Interleukin receptors on astrocytes in the hippocampus are also known to be involved in the development of spatial memories in mice.

www.MedChemExpress.com 59 Interleukin Related Inhibitors & Modulators

Apilimod APY0201 (STA 5326) Cat. No.: HY-14644 Cat. No.: HY-15982

Bioactivity: Apilimod is a potent IL-12/IL-23 inhibitor, and strongly Bioactivity: APY0201 is a potent PIKfyve inhibitor, which inhibits the

inhibits IL-12 with IC50s of 1 nM and 2 nM, in conversion of PtdIns3P to PtdIns(3,5)P 2 in the presence of IFN-γ/SAC-stimulated human PBMCs and SAC-treated monkey 33 in the presence of [ P]ATP with an IC50 of 5.2 nM. APY0201 PBMCs, also inhibits IL-12/IL-23 production. respectively. Purity: 99.49% Purity: 98.0% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

AX-024 AX-024 hydrochloride Cat. No.: HY-107390 Cat. No.: HY-107390A

Bioactivity: AX-024 is an cytokine release inhibitor which can strongly Bioactivity: AX-024 hydrochloride is an cytokine release inhibitor which can inhibit the production of interleukin-6 ( IL-6), tumor strongly inhibit the production of interleukin-6 ( IL-6), necrosis factor-α ( TNFα), interferon-γ ( IFN-γ), IL-10 and tumor necrosis factor-α ( TNFα), interferon-γ ( IFN-γ), IL-17A. IL-10 and IL-17A.

Purity: 98.0% Purity: 99.29% Clinical Data: Phase 1 Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Balsalazide Balsalazide sodium hydrate Cat. No.: HY-B0667 (Balsalazide disodium dihydrate) Cat. No.: HY-B0667A

Bioactivity: Balsalazide could suppress colitis-associated carcinogenesis Bioactivity: Balsalazide sodium hydrate could suppress colitis-associated through modulation of IL-6/STAT3 pathway. carcinogenesis through modulation of IL-6/STAT3 pathway.

Purity: 99.20% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 250 mg, 500 mg 10 mg, 50 mg, 100 mg

Diacerein Eucalyptol (Diacerhein; Diacetylrhein) Cat. No.: HY-N0283 (1,8-Cineole) Cat. No.: HY-N0066

Bioactivity: Diacerein (Diacerhein), a interleukin-1 beta inhibitor, is a Bioactivity: Eucalyptol is an inhibitor of 5-HT3 receptor , potassium slow-acting medicine of the class anthraquinone used to treat channel, TNF-α and IL-1β. joint diseases.

Purity: 98.78% Purity: 98.0% Clinical Data: Launched Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 50 mg

GIBH-130 Ginsenoside Rc Cat. No.: HY-101860 (Panaxoside Rc) Cat. No.: HY-N0042

Bioactivity: GIBH-130 is an effective inhibitor of neuroinflammation. Bioactivity: Ginsenoside Rc, one of major Ginsenosides from Panax ginseng,

GIBH-130 significantly suppresses the IL-1β secretion by enhances GABA receptor A ( GABAA)-mediated ion channel activated microglia ( IC =3.4 nM). 50 currents (I GABA). Ginsenoside Rc inhibits the expression of TNF-α and IL-1β. Purity: 99.82% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg

60 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ginsenoside Rh1 IL-15-IN-1 (Prosapogenin A2; Sanchinoside B2; Sanchinoside Rh1) Cat. No.: HY-N0604 Cat. No.: HY-102049

Bioactivity: Ginsenoside Rh1 (Prosapogenin A2; Sanchinoside B2; Bioactivity: IL-15-IN-1 is a potent and selective Interleukin 15 (IL-15) Sanchinoside Rh1) is isolated from the root of Panax Ginseng. inhibitor, inhibiting the proliferation of IL-15-dependent

Ginsenoside Rh1 inhibits the expression of PPAR-γ, TNF-α, cells with an IC50 of 0.8 μM. IL-6, and IL-1β.

Purity: 98.17% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg 5 mg, 10 mg

IL-17A antagonist 1 IL-17A antagonist 3 Cat. No.: HY-101913 Cat. No.: HY-101915

Bioactivity: IL-17A antagonist 1 is an IL-17A antagonist. Bioactivity: IL-17A antagonist 3 is an IL-17A antagonist.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

IX 207-887 Methylthiouracil Cat. No.: HY-106087 (MTU) Cat. No.: HY-B0513

Bioactivity: IX 207-887 is a novel antiarthritic agent which inhibits the Bioactivity: Methylthiouracil is an antithyroid agent. Methylthiouracil release of interleukin-1 ( IL-1). suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 50 mg, 100 mg

Mulberroside A Neochlorogenic acid Cat. No.: HY-N0619 (trans-5-O-Caffeoylquinic acid) Cat. No.: HY-N0722

Bioactivity: Mulberroside A, the major active anti-tyrosinase compound in Bioactivity: Neochlorogenic acid is a natural polyphenolic compound found the root bark extract of Morus alba L. (Moraceae), is widely in dried fruits and other plants. Neochlorogenic acid inhibits employed as an active ingredient in whitening cosmetics. IC50 the production of TNF-α and IL-1β. Neochlorogenic acid value: 1.29 μmol/L (inhibition of the monophenolase activity); suppresses iNOS and COX-2 protein expression. Neochlorogenic KI value: 0.385 μmol/L (the inhibition constant of the… acid also inhibits phosphorylated NF-κB p65 and p38 MAPK… Purity: 99.53% Purity: 99.46% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg

NFAT Transcription Factor Regulator-1 NO-prednisolone Cat. No.: HY-112778 (NCX-1015) Cat. No.: HY-101757

Bioactivity: NFAT Transcription Factor Regulator-1 is an IL-2 synthesis Bioactivity: NO-prednisolone is a nitric oxide (NO)-releasing derivative of

inhibitor with an IC50 of 182 nM. Prednisolone. NO-prednisolone potently stimulates IL-10 production in vivo.

Purity: 99.37% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 61

Nosantine racemate RCGD423 (NPT-15392 racemate) Cat. No.: HY-101687 Cat. No.: HY-114775

Bioactivity: Nosantine racemate is the racemate of Nosantine. Nosantine is Bioactivity: RCGD423 is a gp130 modulator, which prevents articular an inducer of IL-2 or enhancer of IL-2 induction by cartilage degeneration and promotes repair. phytohemagglutinin (PHA).

Purity: >98% Purity: 99.34% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 20 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

RP-54745 SC144 Cat. No.: HY-101716 Cat. No.: HY-15614

Bioactivity: RP-54745 is an inhibitor of macrophage stimulation and Bioactivity: SC144 is the first-in-class orally active small-molecule gp130 interleukin-1 production, and a potential antirheumatic inhibitor; inhibits cell growth in a panel of human ovarian compound. cancer cell lines with IC50 values in a submicromolar range. IC50 value: < 1 uM (Cell assay) [1] Target: gp130 inhibitor SC144 shows greater potency in human ovarian cancer cell lines… Purity: 99.93% Purity: 98.05% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

SC144 hydrochloride Suplatast Tosilate Cat. No.: HY-15614A (IPD 1151T) Cat. No.: HY-17002

Bioactivity: SC144 hydrochloride is the first-in-class orally active Bioactivity: Suplatast tosilate(IPD 1151T) is a Th2 cytokine inhibitor that small-molecule gp130 inhibitor; inhibits cell growth in a attenuates IL-2, IL-5 and IL-13 production and has no effect panel of human ovarian cancer cell lines with IC50 values in a on IFN-γ production. submicromolar range.

Purity: >98% Purity: 98.09% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Tyrphostin A1 Ustekinumab (Tyrphostin 1; AG9) Cat. No.: HY-16668 (Anti-Human IL-12/IL-23, Human Antibody) Cat. No.: HY-P9909

Bioactivity: Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production Bioactivity: Ustekinumab is an anti- IL-12/ IL-23 IgG1κ human monoclonal in macrophage cultures and antigen-induced generation of Th1 antibody. cells. IC50 value: Target: IL-12 production inhibitor Addition of increasing concentration of A1 resulted in a dose dependent decrease of IL-12 p40, with maximal inhibition (62.5%)… Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg 10 mg, 100 mg

Vadimezan Veledimex (ASA-404; DMXAA) Cat. No.: HY-10964 (INXN-1001; RG-115932) Cat. No.: HY-16785

Bioactivity: Vadimezan (ASA-404; DMXAA), the tumor vascular disrupting Bioactivity: Veledimex is an oral activator ligand for a proprietary gene agent (tumor-VDA), is a murine agonist of the stimulator of therapy promoter system, and a moderate inhibitor of and interferon genes ( STING) and also a potent inducer of type I substrate for CYP3A4/5. IFNs and other cytokines.

Purity: 99.81% Purity: 99.09% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

62 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Veledimex racemate Veledimex S enantiomer (RG-115932 racemate; INXN-1001 racemate) Cat. No.: HY-16785A (INXN-1001 S enantiome; RG-115932 S enantiome) Cat. No.: HY-16785B

Bioactivity: Veledimex racemate is the racemate of veledimex. Veledimex is Bioactivity: Veledimex S enantiomer is the S enantiomer of veledimex. an orally available, small-molecule activator ligand for the Veledimex is an oral activator ligand for a proprietary gene RheoSwitch Therapeutic System. therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5.

Purity: 98.0% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg

VGX-1027 Vidofludimus (GIT 27) Cat. No.: HY-15507 (4sc-101; SC12267) Cat. No.: HY-14908

Bioactivity: VGX-1027(GIT27) is an isoxazole compound that exhibits various Bioactivity: Vidofludimus(4SC-101; SC12267) is a novel immunosuppressive immunomodulatory properties; reduce the secretion of IL-1beta, drug that inhibits DHODH; inhibits IL-17 secretion in vitro TNF-alpha and IL-10 from purified murine macrophages. independently of effects on lymphocyte proliferation.

Purity: 99.92% Purity: 99.14% Clinical Data: Phase 1 Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

Y-320 YM-90709 Cat. No.: HY-15898 Cat. No.: HY-19969

Bioactivity: Y-320 is a new phenylpyrazoleanilide immunomodulator; inhibits Bioactivity: YM-90709 is a novel antagonist which inhibits the binding of IL-17 production by CD4 T cells stimulated with IL-15 with interleukin-5 to interleukin-5 receptor. IC50 values of 20 to 60 nM.

Purity: 99.07% Purity: 99.64% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 63 IRAK Interleukin-1 receptor associated kinase;IL-1R associated kinase

Interleukin-1 receptor-associated kinase (IRAK) is first described as a signal transducer for the proinflammatory cytokine IL-1 and is later implicated in signal transduction of other members of the Toll-like receptor (TLR)/IL-1R family. Four different IRAK-like molecules have been identified: two active kinases, IRAK-1 and IRAK-4, and two inactive kinases, IRAK-2 and IRAK-M. All IRAKs mediate activation of NF-κB and MAPK pathways. IRAKs are protein kinases involved in signalling innate immune responses from TLRs. After TLR-4 and TLR-2 recognize pathogen-associated molecular patterns, such as LPS and peptidoglycan, all IRAK members form multimeric receptor complexes. IRAKs are essential signaling intermediates in the TLR/IL-1R pathway to both IKK and MAPKs activation. These two pathways are central to the activation of several transcription factors, including NF-κB and AP-1, which contribute to the establishment of an immune response.

64 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] IRAK Inhibitors & Modulators

AZ1495 CA-4948 Cat. No.: HY-111101 Cat. No.: HY-109585

Bioactivity: AZ1495 (compound 28) is an oral active inhibitor of Bioactivity: CA-4948 is a selective and potent IRAK4 inhibitor.

Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Shows activity in treatment of mutant MYD88 L265P diff… Purity: 99.83% Purity: 98.44% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

Ginsenoside Rb1 IRAK inhibitor 1 (Gypenoside III) Cat. No.: HY-N0039 Cat. No.: HY-13275

Bioactivity: Ginsenoside Rb1, a main constituent of the root of Panax Bioactivity: IRAK inhibitor 1 is a potent IRAK-4 inhibitor with IC50 of 216 ginseng, inhibits Na+, K+-ATPase activity with an IC of 50 nM, is poorly active against JNK-1 and JNK-2 with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and 3.801 μM, and >10 μM, respectively. phosphorylation of NF-κB p65 . Purity: 98.0% Purity: 99.47% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg

IRAK inhibitor 2 IRAK inhibitor 3 Cat. No.: HY-13276 Cat. No.: HY-13277

Bioactivity: IRAK inhibitor 2 is interleukin-1 receptor associated kinase Bioactivity: IRAK inhibitor 3 is an interleukin-1 (IL-I) inhibitor . receptor-associated kinase ( IRAK) kinase modulator extracted from patent WO2008030579 A2.

Purity: 97.23% Purity: 96.20% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg

IRAK inhibitor 4 IRAK inhibitor 4 trans Cat. No.: HY-13278 Cat. No.: HY-13278A

Bioactivity: IRAK inhibitor 4 is an interleukin-1 receptor associated Bioactivity: IRAK inhibitor 4 (trans) is the trans form of IRAK inhibitor kinase 4( IRAK4) inhibitor. 4. IRAK inhibitor 4 is an interleukin-1 receptor associated kinase 4 ( IRAK4) inhibitor.

Purity: 99.24% Purity: 99.50% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 5 mg

IRAK inhibitor 6 IRAK-1-4 Inhibitor I Cat. No.: HY-13280 (IRAK-1/4 Inhibitor I) Cat. No.: HY-13329

Bioactivity: IRAK inhibitor 6 is an inhibitor of interleukin-1 receptor Bioactivity: IRAK-1-4 Inhibitor I is an inhibitor of interleukin-1

associated kinase 4 (IRAK-4) with IC50 of 160 nM. receptor-associated kinase 1/4 ( IRAK 1/4) with IC50s of 0.2 μM and 0.3 μM, respectively.

Purity: 99.75% Purity: 98.49% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 65

IRAK4-IN-1 PF06650833 Cat. No.: HY-101922 Cat. No.: HY-19836

Bioactivity: IRAK4-IN-1 is an interleukin-1 receptor associated kinase 4 ( Bioactivity: PF06650833 is an inhibitor of Interleukin-1 receptor associated

IRAK4) inhibitor with an IC50 of 7 nM. kinase 4 (IRAK4), and used to treat diseases such as rheumatoid arthritis, lupus, and lymphomas.

Purity: 99.01% Purity: 98.68% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

66 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] MyD88

MyD88 (Myeloid differentiation primary response gene 88) is a protein that, in humans, is encoded by the MYD88 gene. Available evidence suggests that MYD88 is dispensable for human resistance to common viral infections and to all but a few pyogenic bacterial infections, demonstrating a major difference between mouse and human immune responses. MyD88 is an essential adaptor protein in the IL-1R1 signaling pathway. MyD88 may define a family of signal transduction molecules with an ancestral function in the activation of the immune system. MyD88 functions as a pure adaptor linking the IL-1R1 to downstream IRAK kinases. Mutation in MYD88 at position 265 leading to a change from leucine to proline have been identified in many human lymphomas including ABC subtype of Diffuse Large B-cell Lymphoma and Waldenstrom's Macroglobulinemia.

www.MedChemExpress.com 67 MyD88 Inhibitors & Modulators

Schaftoside ST 2825 Cat. No.: HY-N0703 Cat. No.: HY-50937

Bioactivity: Schaftoside is a flavonoid found in a variety of Chinese Bioactivity: ST 2825 is a MyD88 dimerization inhibitor. herbal medicines, such as Eleusine indica. Schaftoside inhibits the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission [1]. Purity: >98% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg

68 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] NO Synthase Nitric oxide synthases;NOS

Nitric oxide synthases (NOSs) are a family of enzymes catalyzing the production of nitric oxide (NO) from L-arginine. NO synthases catalyze the oxidation of L-arginine to NO and L-citrulline. Mammals contain three NOS isoforms: neuronal NOS (nNOS), inducible NOS (iNOS), and endothelial NOS (eNOS). NO produced from these different NOS isoforms is involved in a wide range of physiologic functions in the nervous, immune, and cardiovascular systems. Unregulated NO production can lead to pathologic conditions such as stroke, inflammation, and hypertension. Therefore, the control of NOS activity by isoform selective NOS inhibitors has great potential for therapeutic treatments of NO-related diseases.

www.MedChemExpress.com 69 NO Synthase Inhibitors & Modulators

1400W Dihydrochloride 3',4'-Dihydroxyflavonol Cat. No.: HY-18731 (DiOHF) Cat. No.: HY-111804

Bioactivity: 1400W dihydrochloride is a potent and selective inhibitor of Bioactivity: 3',4'-Dihydroxyflavonol (DiOHF) is an effective antioxidant,

human inducible NO synthase with Ki values of 7 nM. which reduces superoxide and improves nitric oxide ( NO) function in diabetic rat mesenteric arteries [1].

Purity: 99.66% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg 5 mg, 10 mg, 50 mg, 100 mg

6-Biopterin Agmatine sulfate (L-Biopterin) Cat. No.: HY-102015 Cat. No.: HY-101238

Bioactivity: 6-Biopterin (L-Biopterin), a pterin derivative, is a NO Bioactivity: Agmatine sulfate exerts modulatory action at multiple synthase cofactor. molecular targets, such as neurotransmitter systems, ion channels and nitric oxide synthesis. It is an endogenous agonist at imidazoline receptor and a NO synthase inhibitor. Purity: 98.02% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg, 500 mg, 1 g

Asymmetric dimethylarginine AVE-3085 Cat. No.: HY-113216 Cat. No.: HY-19504

Bioactivity: Asymmetric dimethylarginine is an endogenous inhibitor of Bioactivity: AVE-3085 is a potent endothelial nitric oxide synthase nitric oxide synthase (NOS), and functions as a marker of enhancer, used for cardiovascular disease treatment. endothelial dysfunction in a number of pathological states.

Purity: 98.0% Purity: 99.0% Clinical Data: Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 1 mg, 5 mg, 10 mg, 20 mg

Bendazol Chondroitin sulfate Cat. No.: HY-B2141 (Chondroitin polysulfate) Cat. No.: HY-B2162

Bioactivity: Bendazol is a hypotensive drug which can also enhance NO Bioactivity: Chondroitin sulfate, one of five classes of synthase activity in renal glomeruli and collecting tubules. glycosaminoglycans, has been widely used in the treatment of osteoarthritis. Chondroitin sulfate reduces inflammation mediators and the apoptotic process and is able to reduce protein production of inflammatory cytokines, iNOS and MMPs Purity: 99.45% Purity: 95.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 250 mg, 1 g 100 mg, 500 mg, 1 g

Ginsenoside C-K Ginsenoside Rb3 (Ginsenoside K; Ginsenoside compound K) Cat. No.: HY-N0904 (Gypenoside IV) Cat. No.: HY-N0041

Bioactivity: Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits Bioactivity: Ginsenoside Rb3 is extracted from steamed Panax notoginseng. anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced

Ginsenoside C-K exhibits an inhibition against the activity of NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T CYP2C9 and CYP2A6 in human liver microsomes with IC s of 50 cell lines. Ginsenoside Rb3 also inhibits the induction of 32.0±3.6 μM and 63.6±4.2 μM, respectively. COX-2 and iNOS mRNA. Purity: 98.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg 5 mg, 10 mg

70 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

GW274150 Kuwanon A Cat. No.: HY-12119 Cat. No.: HY-N2300

Bioactivity: GW274150 is a novel arginine-competitive, NADPH-dependent iNOS Bioactivity: Kuwanon A is a flavone derivative isolated from the root barks inhibitor that has been identified from a series of acetamide of the mulberry tree ( Morus alba L.); inhibits nitric oxide

amino acids that have a high selectivity for iNOS vs both eNOS production with an IC50 of 10.5 μM. (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration. Target:… Purity: 99.84% Purity: 96.30% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg 2 mg, 5 mg, 10 mg, 25 mg

L-Arginine L-Arginine hydrochloride ((S)-(+)-Arginine) Cat. No.: HY-N0455 ((S)-(+)-Arginine hydrochloride) Cat. No.: HY-N0455A

Bioactivity: L-Arginine is the nitrogen donor for synthesis of nitric Bioactivity: L-Arginine is the nitrogen donor for synthesis of nitric oxide, a potent vasodilator that is deficient during times of oxide, a potent vasodilator that is deficient during times of sickle cell crisis. Target: Others L-Arginine is an α-amino sickle cell crisis. Target: Others Arginine is an α-amino acid. It was first isolated in 1886. The L-form is one of the acid. It was first isolated in 1886. The L-form is one of the 20 most common natural amino acids. At the level of molecular… 20 most common natural amino acids. At the level of molecular… Purity: 98.0% Purity: 98.0% Clinical Data: Phase 4 Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 1 g, 5 g, 100 g, 500 g 1 g, 5 g

L-Canavanine sulfate L-NAME hydrochloride Cat. No.: HY-B1581A (NG-Nitroarginine methyl ester hydrochloride) Cat. No.: HY-18729A

Bioactivity: L-Canavanine sulfate is a selective inhibitor of inducible NO Bioactivity: L-NAME hydrochloride inhibits NOS with an IC50 of 70 μM. synthase. L-NAME is a precursor to NOS inhibitor L-NOARG which has an

IC50 value of 1.4 μM.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 50 mg, 100 mg 100 mg, 500 mg

L-NIL L-NIO dihydrochloride Cat. No.: HY-12116 Cat. No.: HY-100986

Bioactivity: L-NIL is a potent and selective inhibitor of inducible NO Bioactivity: L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with synthase with IC50s of 3.3 and 92 μM for mouse inducible NO K s of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial synthase and rat brain constitutive NO synthase, respectively. i (eNOS), and inducible (iNOS), respectively [1] [2]. L-… Purity: 99.26% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 50 mg, 100 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg

L-NMMA acetate Piceatannol 3'-O-glucoside (Tilarginine acetate; Methylarginine acetate) Cat. No.: HY-18732A (Quzhaqigan) Cat. No.: HY-N2237

Bioactivity: L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS Bioactivity: Piceatannol 3'-O-glucoside, an active component of Rhubarb,

isoforms including NOS1, NOS2, and NOS3. The Ki values for activates endothelial nitric oxide ( NO) synthase through inhibition of arginase activity with IC s of 11.22 µM and nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 50 0.18, 0.4, and 6 µM, respectively. 11.06 µM against arginase I and arginase II, respectively.

Purity: 98.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 5 mg 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 71

Prim-O-glucosylcimifugin S-MTC Cat. No.: HY-N0635 Cat. No.: HY-U00432

Bioactivity: Prim-O-glucosylcimifugin exerts anti-inflammatory effects Bioactivity: S-MTC is a selective type I nitric oxide synthase ( NOS) through the inhibition of iNOS and COX-2 expression by through inhibitor. regulating JAK2/STAT3 signaling.

Purity: 99.76% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 5 mg, 10 mg, 25 mg

Syzalterin Tetrahydrobiopterin Cat. No.: HY-N1187 (Sapropterin) Cat. No.: HY-107383

Bioactivity: Syzalterin is an inhibitor of NO production with an IC50 of Bioactivity: Tetrahydrobiopterin is a cofactor of the aromatic amino 1.87 μg/mL. acid hydroxylases enzymes and also acts as an essential cofactor for all nitric oxide synthase (NOS) isoforms.

Purity: >98% Purity: 98.63% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

72 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] NOD-like Receptor (NLR)

Nucleotide oligomerization domain (NOD)-like receptors (NLRs) are a specialized group of intracellular proteins that play a critical role in the regulation of the host innate immune response. NLRs act as scaffolding proteins that assemble signaling platforms that trigger nuclear factor-κB and mitogen-activated protein kinase signaling pathways and control the activation of inflammatory caspases. Importantly, mutations in several members of the NLR family have been linked to a variety of inflammatory diseases consistent with these molecules playing an important role in host-pathogen interactions and the inflammatory response. NLRs including Nod1 and Nod2 are thought to be kept in an inactive state by intra-molecular interactions. The central role of the Nod-like receptor (NLR) protein family became increasingly appreciated in innate immune responses. NLRs are classified as part of the signal transduction ATPases with numerous domains (STAND) clade within the AAA+ ATPase family.

www.MedChemExpress.com 73 NOD-like Receptor (NLR) Inhibitors & Modulators

Arglabin CY-09 ((+)-Arglabin) Cat. No.: HY-16059 Cat. No.: HY-103666

Bioactivity: Arglabin is a sesquiterpene gamma-lactone is isolated from Bioactivity: CY-09 is an NLRP3 inhibitor. Artemisia glabella; anticancer natural compound.

Purity: 99.17% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Dapansutrile INF39 (OLT1177) Cat. No.: HY-17629 Cat. No.: HY-101868

Bioactivity: Dapansutrile (OLT1177) is a potent, selective and orally Bioactivity: INF39 is an irreversible and noncytotoxic NLRP3 inhibitor. active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity [1].

Purity: 98.0% Purity: 99.61% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg

MCC950 MCC950 sodium (CP-456773) Cat. No.: HY-12815 (CP-456773 sodium; CRID3 sodium salt) Cat. No.: HY-12815A

Bioactivity: MCC950 is a potent and selective NLRP3 inhibitor with IC50s Bioactivity: MCC950 sodium is a potent, selective NLRP3 inhibitor with IC s of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively. of 7.5 and 8.1 nM in BMDMs and HMDMs, respectively. 50

Purity: 98.0% Purity: 99.43% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in Water, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

N4-Acetylcytidine triphosphate NOD-IN-1 (ac4CTP) Cat. No.: HY-111815 Cat. No.: HY-100691

Bioactivity: N4-Acetylcytidine triphosphate is a endogenous nucleoside Bioactivity: NOD-IN-1 is a potent mixed inhibitor of nucleotide-binding metabolite from the degradation of tRNA, primes and activates oligomerization domain ( NOD)-like receptors, NOD1 and NOD2, [1] NLRP3 inflammation by inducing HMGB1 expression . with IC50 of 5.74 μM and 6.45 μM, respectively.

Purity: >98% Purity: 98.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Nodinitib-1 Ruscogenin (ML130; CID-1088438) Cat. No.: HY-18639 Cat. No.: HY-N0496

Bioactivity: Nodinitib-1 (ML130;CID-1088438) is a NOD1 inhibitor with an Bioactivity: Ruscogenin, an important steroid sapogenin derived from

IC50 of 0.56 μM. Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway and exerts significant anti-inflammatory and anti-thrombotic activities… Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

74 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Troxerutin (Trihydroxyethylrutin) Cat. No.: HY-N0139

Bioactivity: Troxerutin, also known as vitamin P4, is a tri-hydroxyethylated derivative of natural bioflavonoid rutins which can inhibit the production of reactive oxygen species ( ROS) and depress ER stress-mediated NOD activation.

Purity: 98.05% Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, 100 mg, 5 g

www.MedChemExpress.com 75 PD-1/PD-L1 PD-1/Programmed death-ligand 1

Programmed death-1 (PD-1) is a receptor on T cells that has been shown to suppress activating signals from the T cell receptor when bound by either of its ligands, Programmed death-ligand 1 (PD-L1) or PD-L2. When PD-1 expressing T cells contact cells expressing its ligands, functional activities in response to antigenic stimuli, including proliferation, cytokine secretion, and cytotoxicity are reduced. PD-1/PD-Ligand interactions down regulate immune responses during resolution of an infection or tumor, or during the development of self tolerance. Interference with the PD-1/PD-L1 interaction has also shown enhanced T cell activity in chronic infection systems. Chronic lymphocytic chorio meningitis virus infection of mice also exhibits improved virus clearance and restored immunity with blockade of PD-L1. In addition to enhancing immunologic responses to chronic antigens, blockade of the PD-1/PD-L1 pathway has also been shown to enhance responses to vaccination, including therapeutic vaccination in the context of chronic infection.

76 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] PD-1/PD-L1 Inhibitors & Modulators

Atezolizumab Avelumab (Anti-Human PD-L1, Human Antibody; MSB 0010718C; (MPDL3280A) Cat. No.: HY-P9904 MSB0010718C) Cat. No.: HY-108730

Bioactivity: Atezolizumab is a selective humanized monoclonal IgG1 antibody Bioactivity: Avelumab is a fully human IgG1 anti-PD-L1 monoclonal antibody against programmed death ligand 1 ( PD-L1), used for cancer with potential antibody-dependent cell-mediated cytotoxicity. research.

Purity: 98.98% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg, 25 mg Size: 1 mg, 5 mg, 20 mg

BMS-1 BMS-1166 (PD-1/PD-L1 inhibitor 1) Cat. No.: HY-19991 Cat. No.: HY-102011

Bioactivity: BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein Bioactivity: BMS-1166 is a potent PD-1/PD-L1 interaction inhibitor with an [1] [2] IC of 1.4 nM. interaction (IC 50 between 6 and 100 nM) . 50

Purity: 99.61% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

BMS-202 Durvalumab (PD-1/PD-L1 inhibitor 2) Cat. No.: HY-19745 (MEDI 4736) Cat. No.: HY-P9919

Bioactivity: BMS-202 is an inhibitor of the PD-1/PD-L1 protein/protein Bioactivity: Durvalumab (MEDI 4736) is an humanized anti- PD-L1 monoclonal

interaction with an IC50 of 18 nM. antibody. Durvalumab blocks the interaction of PD-L1 with PD-1 and CD80 [1].

Purity: 99.37% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 1 mg, 5 mg

Nivolumab NP-12 (BMS-936558; ONO-4538; MDX-1106) Cat. No.: HY-P9903 Cat. No.: HY-P1812

Bioactivity: Nivolumab is a programmed death receptor-1 ( PD-1) blocking Bioactivity: NP-12 is a peptide antagonist of the PD-1 signaling pathway, antibody to treat advanced (metastatic) non-small cell lung which acts as an immunomodulatory agent for cancer therapy cancer. [1].

Purity: 98.56% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 1 mg, 5 mg Size:

PD-1-IN-1 PD-1-IN-17 Cat. No.: HY-101093 Cat. No.: HY-101097

Bioactivity: PD-1-IN-1 is an inhibitor of programmed cell dealth-1 ( PD-1) Bioactivity: PD-1-IN-17 is a programmed cell death- 1 (PD-1) inhibitor extracted from patent WO 2015033299 A1, compound example 4. extracted from patent WO2015033301A1, Compound 12, inhibits 92% splenocyte proliferation at 100 nM [1].

Purity: 98.48% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg

www.MedChemExpress.com 77

PD-1-IN-17 TFA PD-1-IN-18 Cat. No.: HY-101097A Cat. No.: HY-101098

Bioactivity: PD-1-IN-17 TFA is a programmed cell death- 1 (PD-1) inhibitor Bioactivity: PD-1-IN-18 is a PD1 signaling pathway inhibitor, which acts extracted from patent WO2015033301A1, Compound 12, inhibits as an immunomodulator. 92% splenocyte proliferation at 100 nM [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg Size: 250 mg, 500 mg

PD-1-IN-20 PD-1-IN-22 Cat. No.: HY-101093B Cat. No.: HY-128605

Bioactivity: PD-1-IN-20 is a PD-1 inhibitor. Bioactivity: PD-1-IN-22 is a potent programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1) interaction [1] inhibitor with an IC50 of 92.3 nM .

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 500 mg, 250 mg Size: 100 mg, 250 mg, 500 mg

Pembrolizumab Sulfamethizole (MK-3475; Lambrolizumab) Cat. No.: HY-P9902 Cat. No.: HY-B0333

Bioactivity: Pembrolizumab is a humanized antibody inhibiting the Bioactivity: Sulfamethizole is a sulfathiazole antibacterial agent. Target: programmed cell death 1 ( PD-1) receptor, used in cancer Antibacterial Sulfamethizole is a sulfathiazole antibacterial immunotherapy. agent. Sulfamethizole is a competitive inhibitor of bacterial para-aminobenzoic acid (PABA), a substrate of the enzyme dihydropteroate synthetase. The inhibited reaction is… Purity: >98% Purity: 99.71% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10mM x 1mL in DMSO, 500 mg

Sulfamethoxypyridazine Cat. No.: HY-B1387

Bioactivity: Sulfamethoxypyridazine is a long-acting sulfonamide antibiotic, for treatment of Dermatitis herpetiformis.

Purity: 99.01% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 100 mg

78 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] PGE synthase Prostaglandin E synthase

PGE synthase (Prostaglandin E synthase), which converts cyclooxygenase (COX)-derived prostaglandin (PG) H2 to PGE2, occurs in multiple forms with distinct enzymatic properties, modes of expression, cellular and subcellular localizations and intracellular functions. Cytosolic PGES (cPGES) is a cytosolic protein that is constitutively expressed in a wide variety of cells and tissues and is associated with heat shock protein 90 (Hsp90). Membrane-associated PGES (mPGES), the expression of which is stimulus-inducible and is downregulated by anti-inflammatory glucocorticoids, is a perinuclear protein belonging to the microsomal glutathione S-transferase (GST) family. These two PGESs display distinct functional coupling with upstream COXs in cells; cPGES is predominantly coupled with the constitutive COX-1, whereas mPGES is preferentially linked with the inducible COX-2. Several cytosolic GSTs also have the capacity to convert PGH2 to PGE2 in vitro. Accumulating evidence has suggested that mPGES participates in various pathophysiological states in which COX-2 is involved, implying that mPGES represents a potential novel target for drug development.

www.MedChemExpress.com 79 PGE synthase Inhibitors & Modulators

Benzydamine hydrochloride Bismuth Subsalicylate Cat. No.: HY-30235A (Bismuth oxysalicylate; Bismuth(III) salicylate basic) Cat. No.: HY-B0550

Bioactivity: Benzydamine Hcl is a locally-acting nonsteroidal Bioactivity: Bismuth Subsalicylate is the active ingredient in Pepto-Bismol anti-inflammatory drug with local anaesthetic and analgesic and inhibits prostaglandin G/H Synthase 1/2. Target: Others properties; selectively binds to prostaglandin synthetase and Bismuth Subsalicylate reduces inflammation/irritation of has notable in vitro antibacterial activity. stomach and intestinal lining through inhibition of prostaglandin G/H Synthase 1/2 [1]. Bismuth Subsalicylate is… Purity: 98.79% Purity: Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 5 g, 10 g 100 mg

Flurbiprofen HPGDS inhibitor 1 (dl-Flurbiprofen) Cat. No.: HY-10582 Cat. No.: HY-10439

Bioactivity: Flurbiprofen is a nonsteroidal anti-inflammatory agent (NSAIA) Bioactivity: HPGDS inhibitor 1 is a novel and selective Hematopoietic with antipyretic and analgesic activity. Target: PGE synthase Prostaglandin D Synthase (HPGDS) inhibitor with an IC50 Value Flurbiprofen, a propionic acid derivative, is a nonsteroidal of 0.7 nM. anti-inflammatory agent (NSAIA) with antipyretic and analgesic activity. Oral formulations of flurbiprofen may be used for… Purity: 99.85% Purity: 99.32% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg

HPGDS inhibitor 2 hPGDS-IN-1 Cat. No.: HY-126134 Cat. No.: HY-12791

Bioactivity: HPGDS inhibitor 2 is a highly potent and selective Bioactivity: hPGDS-IN-1 is a hPGDS inhibitor ,with IC50 of 12 nM in the hematopoietic prostaglandin D synthase (H-PGDS) inhibitor Fluorescence Polarization Assay or the EIA assay. IC50 value: [1] 12 nM Target: hPGDS The detailed information please refer to with an IC50 of 9.9 nM . WO2011044307A1 and WO2010080563A2

Purity: >98% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

HQL-79 Limaprost Cat. No.: HY-108259 (17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206) Cat. No.: HY-B0683

Bioactivity: HQL-79 is a potent, selective and orally active human Bioactivity: Limaprost(OP1206) is a PGE1 analog and potent platelet hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, adhesion inhibitor.

highly selectively inhibits the synthesis of PGD 2, and acts

as an anti-allergic agent, with a Kd of 0.8 μM and an IC50<… Purity: 99.0% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg

MF63 PGS-IN-1 Cat. No.: HY-13283 (KME-4) Cat. No.: HY-101587

Bioactivity: MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM Bioactivity: PGS-IN-1 is a potent inhibitor of prostaglandin synthetase

and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, (PGS) with an IC50 of 0.28 μM; also inhibits 5-lipoxygenase respectively. with an IC50 of 1.05 μM.

Purity: 98.94% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 mg, 5 mg, 10 mg, 20 mg 5 mg, 10 mg, 50 mg, 100 mg

80 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Pranoprofen Sinensetin Cat. No.: HY-B0336 (Pedalitin permethyl ether) Cat. No.: HY-N0297

Bioactivity: Pranoprofen is a non-steroidal anti-inflammatory drug used in Bioactivity: Sinensetin is a methylated flavone found in certain citrus ophthalmology. fruits. pocess potent antiangiogenesis and anti-inflammatory, sinensetin enhances adipogenesis and lipolysis. In vitro: Sinensetin promots adipogenesis in 3T3-L1 preadipocytes growing in incomplete differentiation medium, sinensetin… Purity: 98.48% Purity: 99.22% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 25 mg

Suprofen Zomepirac sodium salt (TN-762) Cat. No.: HY-B0270 (McN-2783-21-98) Cat. No.: HY-B0890

Bioactivity: Suprofen (TN-762) is a non-steroidal anti-inflammatory drug Bioactivity: Zomepirac sodium salt is a pyrrole-acetic acid structurally (NSAID). related to tolmetin sodium; a prostaglandin synthetase inhibitor.

Purity: 99.44% Purity: 99.45% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg 100 mg, 500 mg

www.MedChemExpress.com 81 Reactive Oxygen Species

82 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Reactive Oxygen Species Inhibitors & Modulators

(+)-α-Tocopherol (-)-Epigallocatechin Gallate (D-α-Tocopherol; α-Vitamin E) Cat. No.: HY-N0683 (EGCG; Epigallocatechol Gallate) Cat. No.: HY-13653

Bioactivity: (+)-α-Tocopherol is a vitamin E derivative. vitamin E is a Bioactivity: (-)-Epigallocatechin Gallate is a tea flavonoid with potent fat-soluble antioxidant. antioxidant, antiinflammatory, and anticarcinogenic properties. (-)-Epigallocatechin Gallate is reported to inhibit EGFR signaling and thereby exert anticancer effects.

Purity: 98.0% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 1 g 50 mg, 100 mg

(20S)-Protopanaxadiol (±)-Carnitine chloride (20-Epiprotopanaxadiol; 20(S)-APPD) Cat. No.: HY-N0797 (DL-Carnitine chloride) Cat. No.: HY-B1453

Bioactivity: (20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon Bioactivity: (±)-Carnitine chloride exists in two isomers, known as D and metabolic derivative of the protopanaxadiol-type ginseng L. L-carnitine plays an essential role in the β-oxidation of saponin; apoptosis inducer. IC50 value: Target: apoptosis fatty acids and also shows antioxidant, and anti-inflammatory inducer (20S)-Protopanaxadiol was used to induce cytotoxicity activities. for two human glioma cell lines, SF188 and U87MG. For the… Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 5 g

1,3-Dicaffeoylquinic acid 2-Phospho-L-ascorbic acid trisodium salt (L-Ascorbic acid (1,3-O-Dicaffeoylquinic acid; 1,5-Dicaffeoylquinic acid) Cat. No.: HY-N1412 2-phosphate trisodium salt; …) Cat. No.: HY-107837

Bioactivity: 1,3-Dicaffeoylquinic acid is a caffeoylquinic acid derivative Bioactivity: 2-Phospho-L-ascorbic acid trisodium salt acts as an that exhibits antioxidant activity and radical scavenging antioxidant and a stimulator of hepatocyte growth factor activity. (HGF) production.

Purity: 99.82% Purity: 99.36% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg 1 g

3,5-Dicaffeoylquinic acid 3-Indolepropionic acid (3,5-CQA; Isochlorogenic acid A) Cat. No.: HY-N0056 Cat. No.: HY-W015229

Bioactivity: 3,5-Dicaffeoylquinic acid is a natural phenolic acid with Bioactivity: 3-Indolepropionic acid is shown to be a powerful antioxidant antioxidant and anti-inflammatory activities . and has potential in the treatment for Alzheimer’s disease.

Purity: 98.71% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 g

AKBA Albiflorin (Acetyl-11-keto-β-boswellic acid) Cat. No.: HY-N0892 Cat. No.: HY-N0037

Bioactivity: Acetyl-11-Keto-β-Boswellic Acid (AKBA) is an active Bioactivity: Albiflorin is a major constituent contained in peony root; triterpenoid compound from the extract of Boswellia serrate; a possesses therapeutic potential for neurodegenerative novel Nrf2 activator. IC50 value: Target: Nrf2 activator in diseases. IC50 value: Target: in vitro: Albiflorin vitro: AKBA significantly reduced infarct volumes and significantly ameliorated Glu-induced reduction of cell apoptotic cells, and also increased neurologic scores by… viability, nuclear and mitochondrial apoptotic alteration,… Purity: 99.71% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg

www.MedChemExpress.com 83

Allylthiourea alpha-Mangostin (Thiosinamine; N-Allylthiourea) Cat. No.: HY-B0543 (α-Mangostin) Cat. No.: HY-N0328

Bioactivity: Allylthiourea is a metabolic inhibitor that selective inhibits Bioactivity: Alpha-mangostin is a dietary xanthone with broad biological ammonia oxidation. Target: Others Allylthiourea selectively activities, such as antioxidant, anti-allergic, antiviral, inhibits ammonia oxidation at concentrations 8-80 μM. antibacterial, anti-inflammatory and anticancer effects. It is

Allylthiourea (1 μM)inhibits ammonia oxidation by 80%. an inhibitor of mutant IDH1 ( IDH1-R132H) with a Ki of 2.85 … Complete inhibition is observed at an Allylthiourea… Purity: 99.0% Purity: 98.59% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g 10 mg, 25 mg, 50 mg, 100 mg

Amentoflavone Apigenin 7-glucoside (Didemethyl-ginkgetin) Cat. No.: HY-N0662 (Apigenin-7-O-β-D-glucopyranoside; Apigetrin; Cosmosiin) Cat. No.: HY-N0578

Bioactivity: Amentoflavone is a natural biflavone compound with many Bioactivity: Apigenin-7-glucoside exhibits significant anti-proliferative biological properties, including anti-inflammatory, and antioxidant activity, scavengers of ROS. In vitro: antioxidative, and neuroprotective effects. IC50 value: exhibits significant anti-proliferative activity against Target: In vitro: In irradiated v79 cells, Pretreatment with B16F10 melanoma cells after 24 and 48 h of incubation. amentoflavone 24 hours prior to 8 Gy 60Co γ-ray irradiation… Apigenin-7-glucoside provoks an increase of subG0/G1, S and… Purity: 99.80% Purity: 99.88% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg

Ascorbyl palmitate (L-Ascorbic acid 6-hexadecanoate; Asiaticoside 6-O-Palmitoyl-L-ascorbic acid) Cat. No.: HY-B0987 (Madecassol) Cat. No.: HY-N0439

Bioactivity: Ascorbyl palmitate is an ester formed from ascorbic acid and Bioactivity: Asiaticoside, a trisaccaride triterpene from Centella asiatica, palmitic acid creating a fat-soluble form of vitamin C, it is suppresses TGF-β/Smad signaling through inducing Smad7 and also used as an antioxidant food additive. inhibiting TGF-βRI and TGF-βRII in keloid fibroblasts; Asiaticoside shows antioxidant, anti-inflammatory, and anti-ulcer properties. Purity: 99.61% Purity: 98.46% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 200 mg, 500 mg 10 mg, 50 mg, 100 mg

Astaxanthin BD-AcAc 2 Cat. No.: HY-B2163 (Ketone Ester) Cat. No.: HY-15344

Bioactivity: Astaxanthin, a red dietary carotenoid isolated from Bioactivity: BD-AcAc 2, added in diet, could elevated mean blood ketone Haematococcus pluvialis, is an inhibitor of PPARγ and a bodies of 3.5 mm and lowered plasma glucose, insulin, and potent antioxidant with antiproliferative, neuroprotective and leptin in animals; ketone ester given orally would delay anti-inflammatory activity [1]. Astaxanthin has potential in CNS-OT seizures in rats breathing hyperbaric oxygen. IC50 the treatment of various diseases, such as cancers and… value: Target: a ketone ester given orally as… Purity: 98.0% Purity: 95.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Benfotiamine Bergenin (S-Benzoylthiamine O-monophosphate) Cat. No.: HY-17374 (Cuscutin) Cat. No.: HY-N0017

Bioactivity: Benfotiamine is a synthetic S-acyl derivative of thiamine Bioactivity: Bergenin, a polyphenol, is a potent antinarcotic agent with (vitamin B1); an antioxidant dietary supplement. IC50 value: antioxidant action. IC50 value: < 2.5 μM (antiplasmodial) Target: Benfotiamine, the lipid-soluble thiamine derivative [3] Target: In vitro: The naloxone-precipitated withdrawal used as a treatment for diabetic neuropathy, can inhibit three symptom (jumping frequency) was significantly ameliorated (50% major pathways(the hexosamine pathway, the advanced glycation… of control group) by administration of bergenin (20 mg/kg) in… Purity: 99.58% Purity: 99.50% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 2 mg, 5 mg, 10 mg, 50 mg

84 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Bromhexine hydrochloride Bufotalin Cat. No.: HY-B0372A Cat. No.: HY-N0878

Bioactivity: Bromhexine Hydrochloride is a medication prescribed for coughs Bioactivity: Bufotalin is a cardiotoxic bufanolide steroid, cardiac which works by dissolving hard phlegm. Target: Others glycoside analogue, secreted by a number of toad species; a Bromhexine is a mucolytic agent used in the treatment of novel anti-osteoblastoma agent. IC50 value: Target: in vitro: respiratory disorders associated with viscid or excessive bufotalin induced osteoblastoma cell death and apoptosis in mucus. In addition, bromhexine has antioxidant properties.… dose- and time-dependent manners. Further, bufotalin induced… Purity: 99.91% Purity: 98.93% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 mg, 10 mg

Butylhydroxyanisole Calycosin-7-O-β-D-glucoside (Butylated hydroxyanisole; BHA; E320) Cat. No.: HY-B1066 Cat. No.: HY-N0520

Bioactivity: Butylhydroxyanisole is an antioxidant, consisting of a mixture Bioactivity: Calycosin-7-O-β-D-glucoside, a melanin biosynthesis inhibitor, of two isomeric organic compounds, used as a food additive is isolated from the methanol extract of astragalus. IC50 preservative value: 68 μM in inhibition of Tyrosinase Target: In vitro: Calycosin-7-O-β-d-glucoside showed a melanin biosynthesis inhibition zone in a culture plate of Streptomyces… Purity: 99.0% Purity: 98.71% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 10 mg, 50 mg

Canthaxanthin Chlorogenic acid (E 161g; all-trans-Canthaxanthin) Cat. No.: HY-B1960 (3-O-Caffeoylquinic acid; Heriguard; NSC-407296) Cat. No.: HY-N0055

Bioactivity: Canthaxanthin is a red-orange carotenoid with various Bioactivity: Chlorogenic acid is a major phenolic compound in coffee and biological activities, such as antioxidant, antitumor tea. It plays several important and therapeutic roles such as properties. antioxidant activity, antibacterial, hepatoprotective, cardioprotective, anti-inflammatory, antipyretic, neuroprotective, anti-obesity, antiviral, anti-microbial,… Purity: 98.0% Purity: 99.29% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 500 mg

Cichoric Acid Coenzyme Q10 (Cichoric acid; Dicaffeoyltartaric acid) Cat. No.: HY-N0457 (Ubiquinone-10; CoQ10) Cat. No.: HY-N0111

Bioactivity: Cichoric Acid, a natural product, is reported to be Bioactivity: Coenzyme Q10 is an essential cofactor of the electron antioxidative. transport chain and a potent antioxidant agent.

Purity: 99.95% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg, 500 mg, 1 g, 5 g 10 mg, 25 mg, 50 mg

Cynarin Cysteamine (β-Mercaptoethylamine; 2-Aminoethanethiol; (Cynarine) Cat. No.: HY-N0359 2-Mercaptoethylamine) Cat. No.: HY-77591A

Bioactivity: Cynarin is an antichoke agent with a variety of biological Bioactivity: Cysteamine is an agent for the treatment of nephropathic activities including antioxidant, antihistamic and antiviral cystinosis and an antioxidant. Target: Others Cysteamine has activities. been shown to increase intracellular glutathione levels in cystinotic cells, thus restoring the altered redox state of the cells. Also increased rates of apoptosis in cystinotic… Purity: 98.0% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg, 25 mg 5 g

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Cysteamine hydrochloride (β-Mercaptoethylamine Hydrochloride; D-(+)-Glucono-1,5-lactone 2-Aminoethanethiol Hydrochloride; …) Cat. No.: HY-77591 (Gluconic acid lactone) Cat. No.: HY-I0301

Bioactivity: Cysteamine Hydrochloride is an agent for the treatment of Bioactivity: D-(+)-Glucono-1,5-lactone is a polyhydroxy (PHA) that is nephropathic cystinosis and an antioxidant. Target: Others capable of metal chelating, moisturizing and antioxidant Cysteamine has been shown to increase intracellular activity. glutathione levels in cystinotic cells, thus restoring the altered redox state of the cells. Also increased rates of… Purity: 98.0% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 g 5 g

D-alpha-Hydroxyglutaric acid disodium salt Dapsone (Disodium (R)-2-hydroxyglutarate) Cat. No.: HY-100542 (4,4′-Diaminodiphenyl sulfone; DDS) Cat. No.: HY-B0688

Bioactivity: D-alpha-Hydroxyglutaric acid disodium salt is a weak Bioactivity: Dapsone is a sulfone active against a wide range of bacteria competitive α-Ketoglutarate( α-KG)-dependent dioxygenase but mainly employed for its actions against mycobacterium

inhibitor with Ki of 10.87±1.85 mM. K i for L-Hydroxyglutaric leprae. Target: Antibacterial Dapsone is an antibacterial most acid (L-2-HG) is 0.628±0.036 mM. commonly used in combination with rifampicin and clofazimine as multidrug therapy (MDT) for the treatment of Mycobacterium… Purity: 98.0% Purity: 99.15% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 10 mg, 25 mg, 50 mg, 100 mg 1 g, 5 g

Disufenton sodium Ebselen (NXY-059) Cat. No.: HY-13244 (SPI-1005; PZ-51; CCG-39161) Cat. No.: HY-13750

Bioactivity: Disufenton sodium (NXY-059) is the disulfonyl derivative of Bioactivity: Ebselen is a small-molecule capsid Inhibitor of HIV-1 the neuroprotective spin trap phenylbutynitrone(PBN), both replication. Target: Ebselen is an organoselenium compound, as NXY-059, its parent PBN and their hydrolysis/oxidation product an inhibitor of HIV-1 capsid CTD dimerization. Ebselen MNT are very powerful scavengers of free radicals. IC50 value: inhibits early viral postentry events of the HIV-1 life cycle Target: Neuroprotectant in vitro: Disufenton sodium is more… by impairing the incoming capsid uncoating process. [1]… Purity: 98.0% Purity: 99.58% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in Water, Size: 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Echinacoside Echinocystic acid Cat. No.: HY-N0020 Cat. No.: HY-N0271

Bioactivity: Echinacoside is a natural polyphenolic compound, has various Bioactivity: Echinocystic acid a pentacyclic triterpene isolated from the kinds of pharmacological activities, such as antioxidative, fruits of Gleditsia sinensis Lam, has potent antioxidant, anti-inflammatory, neuroprotective, hepatoprotective, nitric anti-inflammatory and anti-tumor properties. In vitro: oxide radical-scavenging and vasodilative ones. IC50 value: Echinocystic acid (EA) inhibit the formation of osteoclast. EA Target: in vitro: Echinacoside(ECH) dose dependently inhibited… inhibit RANKL-induced NF-κB activation and ERK phosphorylation… Purity: 99.52% Purity: 98.08% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg

Efaproxiral Efaproxiral sodium (RSR13) Cat. No.: HY-13619 (RSR13 sodium) Cat. No.: HY-13619A

Bioactivity: Efaproxiral is a synthetic allosteric modifier of haemoglobin Bioactivity: Efaproxiral sodium is a synthetic allosteric modifier of (Hb), decreases Hb-oxygen (O2) binding affinity and enhances haemoglobin (Hb), decreases Hb-oxygen (O2) binding affinity oxygenation of hypoxic tumours during radiation therapy. in and enhances oxygenation of hypoxic tumours during radiation vitro: Efaproxiral increases oxygen levels in hypoxic tumor therapy. in vitro: Efaproxiral increases oxygen levels in tissues by binding non-covalently to the hemoglobin tetramer… hypoxic tumor tissues by binding non-covalently to the… Purity: 99.94% Purity: 98.0% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 50 mg

86 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Ellagic acid Emeramide Cat. No.: HY-B0183 (BDTH2) Cat. No.: HY-16739

Bioactivity: Ellagic acid is a natural antioxidant, and acts as a potent Bioactivity: Emeramide is a novel lipid-soluble, thiol-redox antioxidant

and ATP-competitive CK2 inhibitor, with an IC50 of 40 nM and and heavy metal chelator.

a Ki of 20 nM.

Purity: 99.92% Purity: 99.56% Clinical Data: Phase 2 Clinical Data: Launched Size: 1 g, 5 g Size: 10mM x 1mL in DMSO, 100 mg, 500 mg

Epiberberine chloride Ethoxyquin Cat. No.: HY-N0226A Cat. No.: HY-B1425

Bioactivity: Epiberberine chloride is an alkaloid isolated from Coptis Bioactivity: Ethoxyquin is an antioxidant which has been used in animal chinensis, acts as a potent AChE and BChE inhibitor, and a feed for many years and also an inhibitor of heat shock

non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and protein 90 ( Hsp90). 8.55 μM, respectively. Epiberberine chloride has antioxid…

Purity: 99.60% Purity: 98.05% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 1 g

Ethyl ferulate Eugenol Cat. No.: HY-N0061 Cat. No.: HY-N0337

Bioactivity: Ethyl ferulate, a naturally lipophilic derivative of ferulic Bioactivity: Eugenol is an essential oil found in cloves with acid originally derived from giant fennel ( F. communis), antibacterial, anthelmintic and antioxidant activity. Eugenol induces heme oxygenase-1 (HO-1) and protects rat neurons is shown to inhibit lipid peroxidation. against oxidative stress [1]. Ethyl ferulate also protects neurons against amyloid β peptide (1-42)-induced oxidative… Purity: 99.14% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 100 mg, 500 mg

Ferulic acid sodium Gallic acid (Sodium ferulate) Cat. No.: HY-N0060A (3,4,5-Trihydroxybenzoic acid) Cat. No.: HY-N0523

Bioactivity: Ferulic acid (4-hydroxy-3-methoxycinnamic acid) is a phenolic Bioactivity: Gallic acid is an antioxidant which can inhibit both COX-2. compound present in several plants with claimed beneficial effects in prevention and treatment of disorders linked to oxidative stress and inflammation. IC50 value: Target: 5-HT Receptor In vitro: In the present study we have showed that… Purity: 99.74% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g, 5 g 100 mg, 500 mg

Glabridin Glucoraphanin Cat. No.: HY-N0393 Cat. No.: HY-N4068

Bioactivity: Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds Bioactivity: Glucoraphanin, a natural glucosinolate found in cruciferous

to and activates PPARγ, with an EC50 of 6115 nM. Glabridin vegetable, is a stable precursor of the Nrf2 inducer exhibits antioxidant, anti-bacterial, anti-nephritic, sulforaphane, which possesses antioxidant, anti-inflammatory, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, and anti-carcinogenic effects. antiosteoporotic, cardiovascular protective, neuroprotective… Purity: 99.98% Purity: 99.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg 5 mg, 10 mg

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Glucosamine hydrochloride (D-(+)-Glucosamine hydrochloride; Glutathione oxidized Chitosamine hydrochloride) Cat. No.: HY-N0733 (L-Glutathione oxidized; GSSG) Cat. No.: HY-D0844

Bioactivity: Glucosamine (hydrochloride) is a natural product. IC50 value: Bioactivity: Glutathione oxidized is produced by the oxidation of Target: In vitro: Glucosamine hydrochloride exhibited glutathione which is a major intracellular antioxidant and dose-dependent DPPH antioxidant activity [1]. Short-term (4 h) detoxifying agent. glucosamine hydrochloride treatment inhibited HIF-1α at the protein level, decreased phosphorylation of p70S6K and S6,… Purity: 98.0% Purity: 98.30% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in Water, 50 mg 100 mg

H2DCFDA Hesperidin (DCFH-DA; 2',7'-Dichlorodihydrofluorescein diacetate) Cat. No.: HY-D0940 (Hesperetin 7-rutinoside) Cat. No.: HY-15337

Bioactivity: H2DCFDA is a cell-permeable probe used to detect intracellular Bioactivity: Hesperidin (HP) is a bioflavonoid that plays a role in plant reactive oxygen species (ROS). defense and is abundant in citrus species, such as grapefruit, lemon and orange. Hesperidin is used effectively as a supplemental agent in complementary therapy protocols, since it possesses biological and pharmacological properties as an… Purity: 99.82% Purity: 97.00% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g

Hexaconazole Hexahydrocurcumin ((-)-Hexaconazol) Cat. No.: HY-A0278 Cat. No.: HY-N0929

Bioactivity: Hexaconazole is a systemic fungicide used for the control of Bioactivity: Hexahydrocurcumin is a natural compound which posesses many fungi particularly Ascomycetes and Basidiomycetes. In anticancer and anti-inflammatory activities; selective COX-2 vitro: Among the enzymatic antioxidants, superoxide dismutase inhibitor. IC50 value: Target: in vitro: The relative and peroxidase are significantly up-regulated by hexaconazole. antioxidant potencies of ginger compounds decreased in similar [1] Hexaconazole and its enantiomers cause the down-regulation… order of 1-dehydro-[6]-gingerdione,… Purity: 98.02% Purity: 98.58% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg, 1 g, 5 g 5 mg

HO-1-IN-1 HO-1-IN-1 hydrochloride Cat. No.: HY-111798 Cat. No.: HY-111798A

Bioactivity: HO-1-IN-1 (Compound 2) is a heme oxygenase 1 ( HO-1) Bioactivity: HO-1-IN-1 hydrochloride (Compound 2) is a heme oxygenase 1 ( [1] HO-1) inhibitor with an IC of 250 nM [1]. inhibitor with an IC50 of 250 nM . 50

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

HTHQ Isoquercitrin (1-O-hexyl-2,3,5-trimethylhydroquinone) Cat. No.: HY-100768 (Isoquercitroside; Isoquercetin) Cat. No.: HY-N0768

Bioactivity: HTHQ, which is a hydroquinone monoalkyl ether, is a potent Bioactivity: Isoquercitrin is an effective antioxidant and an eosinophilic anti-oxidative agent, even at low dose levels. HTHQ is found inflammation suppressor. to be a potent anti-lipid-peroxidative compound and its antioxidation activity to be extremely elevated in biological systems, such as that of liver microsomes via the generation… Purity: 99.65% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

88 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Isosteviol L-Ascorbic acid ((-)-Isosteviol; iso-Steviol) Cat. No.: HY-N0872 (L-Ascorbate; Vitamin C) Cat. No.: HY-B0166

Bioactivity: Isosteviol is a derivative of stevioside, a constituent of Bioactivity: L-Ascorbic acid is an effective reducing agent and donor Stevia rebaudiana, which is commonly used as a noncaloric antioxidant. sugar substitute in Japan and Brazil. Target: Isosteviol dose-dependently relaxed the vasopressin (10-8 M)-induced vasoconstriction in isolated aortic rings with or without… Purity: 98.0% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 5 mg, 10 mg 1 g

L-Ascorbic acid sodium salt ((+)-Sodium L-ascorbate; Vitamin L-Glutathione reduced C sodium salt; Sodium L-ascorbate) Cat. No.: HY-B0166A (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) Cat. No.: HY-D0187

Bioactivity: L-Ascorbic acid (sodium) is a more bioavailable form of Bioactivity: L-Glutathione reduced (GSH; γ-L-Glutamyl-L-cysteinyl-glycine) vitamin C that is an antioxidant agent. is an endogenous antioxidant and is capable of scavenging oxygen-derived free radicals.

Purity: 98.0% Purity: 99.83% Clinical Data: Phase 4 Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 g, 5 g 1 g

Lacidipine Levomefolic acid Cat. No.: HY-B0347 (5-MTHF) Cat. No.: HY-14781

Bioactivity: Lacidipine (Lacipil, Motens) is a L-type calcium channel Bioactivity: Levomefolic acid (5-MTHF) is the natural, active form of folic blocker. Target: Calcium Channel Lacidipine, a novel acid used at the cellular level for DNA reproduction, the third-generation dihydropyridine calcium channel blocker, has cysteine cycle and the regulation of homocysteine among other been demonstrated effective for hypertension. lacidipine functions. IC50 value: Target: Folate analog Levomefolic acid protects HKCs against apoptosis induced by ATP depletion and… has been proposed for treatment of cardiovascular disease and… Purity: 99.78% Purity: 98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg, 100 mg, 200 mg 5 mg, 10 mg, 50 mg

Limonene Lipoic acid Cat. No.: HY-N0544 ((R)-(+)-α-Lipoic acid; R-(+)-Thioctic acid) Cat. No.: HY-18733

Bioactivity: Limonene is a monoterpene in citrus peel oil. A popular Bioactivity: Lipoic acid ((R)-(+)-α-Lipoic acid) is an antioxidant, which disinfectant and food preservative. Antimicrobial activities is an essential cofactor of mitochondrial enzyme complexes. [1]. Anti-proliferative activities [2]. Antioxidant and (R)-(+)-α-Lipoic acid is more effective than racemic Lipoic acid. anti-inflammatory effect [3].

Purity: 95.0% Purity: 99.59% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg 500 mg

Liquiritin Lobetyolin Cat. No.: HY-N0376 Cat. No.: HY-N0327

Bioactivity: Liquiritin is a flavonoid isolated from Glycyrrhiza, acts as an Bioactivity: Lobetyolin is derived from Codonopsis pilosula and has antioxidant and has neuroprotective, anti-cancer and antioxidative effect. anti-inflammatory activity [1] [2].

Purity: 98.07% Purity: 99.88% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg

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Luciferase Lycopene Cat. No.: HY-P1004 Cat. No.: HY-N0287

Bioactivity: Luciferase from Vibrio fischeri has also been used in a study to Bioactivity: Lycopene is naturally occurring carotenoids found in tomato, investigate the sensitivity of dark mutants of various strains tomato products, and in other red fruits and vegetables; of luminescent bacteria to reactive oxygen species. exhibits antioxidant effects.

Purity: >98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 1 mg, 5 mg, 10 mg Size: 5 mg, 10 mg, 25 mg, 50 mg

Methoxy-PMS Methyl gallate (1-Methoxy PMS; 1-Methoxyphenazine methosulfate) Cat. No.: HY-D0937 (Gallincin; NSC 363001) Cat. No.: HY-N2010

Bioactivity: 1-Methoxy PMS is stable electron-transport mediator between Bioactivity: Methyl gallate is a plant phenolic with antioxidant, NAD(P)H and tetrazolium dyes. 1-Methoxy PMS can induce active anticancer, and anti-inflammatory activities. Methyl gallate oxygen formation. also shows bacterial inhibition activity.

Purity: 98.14% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg, 200 mg, 500 mg 5 g

Methyl vanillate Mitoquinone mesylate (Mitoquinone methanesulfonate; MitoQ10 Cat. No.: HY-75342 mesylate; MitoQ mesylate) Cat. No.: HY-100116A

Bioactivity: Methyl vanillate, one of the ingredients in Hovenia dulcis Bioactivity: Mitoquinone mesylate is a TPP-based, mitochondrially Thunb, is a Wnt/β-catenin pathway activator [1]. A targeted antioxidant. benzoate ester that is the methyl ester of vanillic acid. It has a role as an antioxidant and a plant metabolite.

Purity: 98.0% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Phase 4 Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg 1 g

N-Acetylcysteine amide Naringenin Cat. No.: HY-110256 Cat. No.: HY-N0100

Bioactivity: N-Acetylcysteine amide is a cell membranes and blood brain Bioactivity: Naringenin is the predominant flavanone in grapefruit; barrier permeant thiol antioxidant and neuroprotective agent. displays strong anti-inflammatory and antioxidant activities.

Purity: 99.0% Purity: 98.72% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg 100 mg, 500 mg, 1 g, 5 g

Nisoldipine Nitisinone (BAY-k 5552) Cat. No.: HY-17402 (NTBC; Nitisone; SC0735) Cat. No.: HY-B0607

Bioactivity: Nisoldipine(BAY-k 5552; Sular) is a calcium channel blocker Bioactivity: Nitisinone(SC0735) is an inhibitor of the enzyme belonging to the dihydropyridines class, specific for L-type 4-hydroxyphenylpyruvate dioxygenase. Target: Cav1.2 with IC50 of 10 nM. IC50 value: 10 nM Target: L-type 4-Hydroxyphenylpyruvate Dioxygenase Nitisinone is a drug used Cav1.2 Nisoldipine is a potent blocker of L-type calcium to slow the effects of hereditary tyrosinemia type 1. channels. Nisoldipine binds directly to inactive calcium… Nitisinone reduced urinary HGA levels from an average of 4.0… Purity: 98.22% Purity: 99.57% Clinical Data: Launched Clinical Data: Launched Size: 100 mg, 500 mg, 1 g Size: 10mM x 1mL in DMSO, 10 mg, 50 mg

90 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

OBA-09 Octahydrocurcumin Cat. No.: HY-12840 (Hexahydrobisdemethoxycurcumin) Cat. No.: HY-N0894

Bioactivity: OBA-09 is a novel multimodal neuroprotectant oxopropanoyloxy Bioactivity: Octahydrocurcumin is a hydrogenated derivatives of curcumin; benzoic acid (a salicylic acid/pyruvate ester); shows robust metabolite of curcumin. IC50 value: Target: OKT3-induced PBMC protective effects in the postischemic brain. IC50 value: proliferation was inhibited by octahydrocurcumin with IC50 of Target: OBA-09 exhibited antioxidative effects in the 82 uM. The investigated substances with the strongest effect postischemic brain, which was evidenced by remarkable… on radical scavenging were tetrahydro-, hexahydro-, and… Purity: 99.86% Purity: 99.52% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg

Octyl gallate Phillygenin (Phillygenol; Epipinoresinol methyl ether; (n-Octyl gallate; Stabilizer GA 8) Cat. No.: HY-N2011 (+)-Phillygenin) Cat. No.: HY-N0483

Bioactivity: Octyl gallate (Progallin O) is widely used as a food additive, Bioactivity: Phillygenin is an active ingredient from Forsythia with many with antimicrobial and antioxidant activity [1] [2]. Octyl medicinal properties, such as antioxidant, reducing blood gallate (Progallin O) shows selective and sensitive lipid, inhibition of low density lipoprotein oxidation. In vitro : 1) Phillygenin shows a greater inhibition on mouse B16 fluorescent property [2]. melanoma cells potential than vincristine. 2) phillygenin had… Purity: 99.96% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 g 5 mg, 10 mg

Pinocembrin Piperlongumine ((+)-Pinocoembrin; Dihydrochrysin; Galangin flavanone) Cat. No.: HY-N0575 (Piplartine) Cat. No.: HY-N2329

Bioactivity: Pinocembrin ((+)-Pinocoembrin) is a flavonoid found in Bioactivity: Piperlongumine is a natural alkaloid isolated from Piper propolis, acts as a competitive inhibitor of histidine longum Linn [1], possesses ant-inflammatory, decarboxylase, and is an effective anti-allergic agent, with antibacterial, antiangiogenic, antioxidant, antitumor, and antioxidant, antimicrobial and anti-inflammatory properties antidiabetic activities [2]. Piperlongumine induces ROS, … [1]. Purity: 99.26% Purity: 99.19% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 10 mg

Procyanidin B2 Protocatechualdehyde (Proanthocyanidin B2) Cat. No.: HY-N0796 (Catechaldehyde; Protocatechuic aldehyde; Rancinamycin IV) Cat. No.: HY-N0295

Bioactivity: Procyanidin B2 is a natural flavonoid, with anti-cancer, Bioactivity: Protocatechualdehyde (Catechaldehyde), a natural polyphenol antioxidant activities. compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and… Purity: 99.40% Purity: 99.92% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg 100 mg

Protopine Quercitrin (Corydinine) Cat. No.: HY-N0793 (Quercetin 3-rhamnoside) Cat. No.: HY-N0418

Bioactivity: Protopine, an isoquinoline alkaloid contained in plants in Bioactivity: Quercitrin is a natural compound found in Tartary buckwheat northeast Asia. IC50 Value: Target: In vitro: Protopine was with a potential anti-inflammation effect that is used to found to reduce nitric oxide (NO), cyclooxygenase-2 (COX-2), treat heart and vascular conditions. IC50 value: Target: In and prostaglandin E(2) (PGE(2)) production by LPS-stimulated vitro: There were significant increases in caspase-3 activity, Raw 264.7 cells, without a cytotoxic effect. Pre-treatment of… loss of MMP, and increases in the apoptotic cell population in… Purity: 98.04% Purity: 99.12% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

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Reynoutrin Rhein (Quercetin-3-D-xyloside; Reinutrin) Cat. No.: HY-N1354 (Rheic Acid; Rhubarb yellow; Monorhein) Cat. No.: HY-N0105

Bioactivity: Reynoutrin (Quercetin-3-D-xyloside) is a flavonoid from Bioactivity: Rhein is a lipophilic anthraquinone extensively found in Psidium cattleianum, with antioxidant and medicinal herbs, and has many pharmacological effects, radical-scavenging activity [1]. including epatoprotective, nephroprotective, anti-inflammatory, antioxidant, anticancer, and antimicrobial activities. IC50 value: Target: In vitro: Rhein (0.1 and 1… Purity: 97.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 100 mg, 200 mg, 500 mg

Riboflavin Tetrabutyrate Rutin Cat. No.: HY-B2239 (Rutoside; Quercetin 3-O-rutinoside) Cat. No.: HY-N0148

Bioactivity: Riboflavin tetrabutyrate is a lipophilic flavin derivative Bioactivity: Rutin, a naturally occurring flavonoid glycoside, has with antioxidative and lipid peroxide-removing activity. antioxidant, anti-inflammatory, anti-allergic, anti-angiogenic and antiviral properties.

Purity: 98.56% Purity: 98.0% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 g, 10 g

S-Methyl-L-cysteine Salsalate (L-S-Methylcysteine) Cat. No.: HY-B2188 (Salicylsalicylic acid; Disalicylic acid) Cat. No.: HY-B1245

Bioactivity: S-Methyl-L-cysteine is a natural product that acts as a Bioactivity: Salsalate is a nonsteroidal anti-inflammatory drug (NSAID). substrate in the catalytic antioxidant system mediated by Target Salsalate is a medication that belongs to the methionine sulfoxide reductase A (MSRA), with antioxidative, salicylate and non-steroidal anti-inflammatory drug (NSAID) neuroprotective, and anti-obesity activities. classes. Relative to other NSAIDs, Salsalate has a weak inhibitory effect on the cyclooxygenase enzyme and decreases… Purity: 95.0% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 100 mg 100 mg

Schisandrin B Secoisolariciresinol diglucoside (Schizandrin-B; Wuweizisu-B; gamma-Schisandrin) Cat. No.: HY-N0089 (SDG; LGM2605) Cat. No.: HY-105008

Bioactivity: Schisandrin B(Wuweizisu-B) is a dibenzocyclooctadiene Bioactivity: Secoisolariciresinol diglucoside (SDG; LGM2605) is a non-toxic derivative isolated from Fructus Schisandrae, has been shown free radical scavenger and antioxidant, reduces reduces ROS to produce antioxidant effect on rodent liver and heart. IC50 generation. Secoisolariciresinol diglucoside enhances value: Target: in vitro: Schisandrin B exhibits activatation Nrf2 signaling, inhibits myeloperoxidase anti-inflammatory activity through modulation of the… (MPO). Purity: 99.99% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 10 mg, 50 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Silibinin Sinapine thiocyanate (Silybin; Silibinin A; Silymarin I) Cat. No.: HY-13748 Cat. No.: HY-N0450

Bioactivity: Silibinin, an effective anti-cancer and chemopreventive agent, Bioactivity: Sinapine is an alkaloid from seeds of the cruciferous species has been shown to exert multiple effects on cancer cells, which shows favorable biological activities such as including inhibition of both cell proliferation and migration. antioxidant and radio-protective activities. IC50 value: Target: anticancer in vitro: silibinin significantly induced the expression of the non-steroidal… Purity: 98.0% Purity: 98.32% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

92 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

Sinapinic acid Sodium formononetin-3'-sulfonate (Sinapic acid) Cat. No.: HY-W009732 (Sul-F) Cat. No.: HY-13063

Bioactivity: Sinapinic acid (Sinapic acid) is a phenolic compound isolated Bioactivity: Sodium formononetin-3'-sulfonate (Sul-F) is a water-sol. from Hydnophytum formicarum Jack. Rhizome, acts as an derivate of formononetin. IC50 value: Target: Research results [1] showed that treatment with Sul-F significantly prevented the inhibitor of HDAC, with an IC50 of 2.27 mM , and also elevation of ST-segment level, decreased the contents of [2] inhibits ACE-I activity . Sinapinic acid posssess pot… creatine kinase-MB, lactate dehydrogenase, alanine… Purity: 99.61% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg 5 mg, 10 mg

Squalene Succinobucol (Super Squalene; trans-Squalene; AddaVax) Cat. No.: HY-N1214 (AGI-1067; Probucol monosuccinate) Cat. No.: HY-14937

Bioactivity: Squalene is an intermediate product in the synthesis of Bioactivity: Succinobucol is a phenolic antioxidant with anti-inflammatory cholesterol, and shows several pharmacological properties such and antiplatelet effects. as hypolipidemic, hepatoprotective, cardioprotective, antioxidant, and antitoxicant activity.

Purity: 98.0% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Sulcotrione Tetrahydroxyquinone Cat. No.: HY-107368 (Tetrahydroxy-1,4-benzoquinone; Tetrahydroxybenzoquinone) Cat. No.: HY-B1106

Bioactivity: Sulcotrione is a β-triketone herbicide which can inhibit Bioactivity: Tetrahydroxyquinone is a molecule best known as a primitive hydroxyphenylpyruvate dioxygenase ( HPPD). anticataract drug, is also a highly redox active molecule that can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS).

Purity: 99.56% Purity: 95.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg, 100 mg 100 mg

trans-Trimethoxyresveratrol (trans-trismethoxy Resveratrol; Trolox E-Resveratrol Trimethyl Ether; Tri-O-methylresveratrol) Cat. No.: HY-N1408 Cat. No.: HY-101445

Bioactivity: Trans-Trimethoxyresveratrol is a derivative of Resveratrol Bioactivity: Trolox is a vitamin E analogue and is a powerful antioxidant. (RSV),and it may be a more potent anti-inflammatory, antiangiogenic and vascular-disrupting agent when compared with resveratrol. In vitro: The in vitro study of resveratrol and trans-Trimethoxyresveratrol showed rather weak cytotoxic… Purity: 99.72% Purity: 99.53% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 50 mg 500 mg, 1 g, 5 g

UPF-648 Uric acid Cat. No.: HY-15600 Cat. No.: HY-B2130

Bioactivity: UPF-648 is a potent kynurenine 3-monooxygenase (KMO) Bioactivity: Uric acid is an endogenous antioxidant that scavenges reactive inhibitor; exhibits highly active at 1 uM (81 ± 10% KMO oxygen species (ROS) including singlet oxygen, oxygen inhibition); ineffective at blocking KAT activity. IC50 value: radicals, and peroxynitrite. 1 uM(81 ± 10 % inhibition) [1] Target: KMO inhibitor in vitro: BFF 122 inhibited KAT activity almost completely at both 1 and… Purity: 99.12% Purity: 99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 1 g 5 mg, 10 mg

www.MedChemExpress.com 93

Urolithin A Veratric acid Cat. No.: HY-100599 (3,4-Dimethoxybenzoic acid) Cat. No.: HY-N2007

Bioactivity: Urolithin A is an intestinal metabolite of ellagic acid with Bioactivity: Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active antioxidant and antiproliferative effects; inhibits T24 and phenolic compound derived from vegetables and fruits, has [1] [3] Caco-2 cell growth with IC50 values of 43.9 and 49 μM, antioxidant and anti-inflammatory activities . respectively. Veratric acid also acts as a protective agent agai…

Purity: 98.06% Purity: 99.99% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 100 mg

Visomitin Xanthotoxol (SKQ1) Cat. No.: HY-100474 (8-Hydroxypsoralen) Cat. No.: HY-30152

Bioactivity: Visomitin is a new antioxidant with the highest mitochondrion Bioactivity: Xanthotoxol is a biologically active linear furocoumarin, membrane penetrating ability and potent antioxidant shows strong pharmacological activities as anti-inflammatory, capability. antioxidant, 5-HT antagonistic, and neuroprotective effects.

Purity: 98.0% Purity: 99.15% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Zofenopril calcium (SQ26991) Cat. No.: HY-B0655

Bioactivity: Zofenopril Calcium (SQ26991) is an antioxidant that acts as an angiotensin-converting enzyme inhibitor. Target: ACE Zofenopril Calcium is a pro-drug designed to undergo metabolic hydrolysis yielding the active free sulfhydryl compound zofenoprilat, which is an angiotensin converting enzyme (ACE)… Purity: 97.91% Clinical Data: Launched Size: 5 mg, 10 mg, 50 mg, 100 mg

94 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Salt-inducible Kinase (SIK)

Salt-inducible Kinases (SIK) are a family of related serine-threonine kinases. In cultured adrenocortical cells, SIK1 is rapidly but transiently induced by adrenocorticotropin (ACTH) treatment, suggesting that it contributes to ACTH-mediated induction of steroidogenic enzymes. SIK2 is found in adipocytes and phosphorylates a specific serine residue. Members of the SIK family are emerging as important modulators of key processes such as steroid hormone biosynthesis by the adrenal cortex in adipocytes.

www.MedChemExpress.com 95 Salt-inducible Kinase (SIK) Inhibitors & Modulators

ARN-3236 HG-9-91-01 Cat. No.: HY-120856 (SIK inhibitor 1) Cat. No.: HY-15776

Bioactivity: ARN-3236 is an oral active and selective inhibitor of Bioactivity: HG-9-91-01 is a potent and highly selective salt-inducible

salt-inducible kinase 2 (SIK2), with IC50s of <1 nM, 21.63 nM kinase ( SIKs) inhibitor with IC50s of 0.92 nM, 6.6 nM and 9.6 and 6.63 nM for SIK2, SIK1 and SIK3, respectively. Has nM for SIK1, SIK2 and SIK3 respectively. anti-cancer activity [1] [2]. Purity: 98.12% Purity: 98.17% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

YKL-05-099 Cat. No.: HY-101147

Bioactivity: YKL-05-099 is a salt-inducible kinase ( SIK) probe. YKL-05-099

binds to SIK1 and SIK3 with IC50s of ~10 and ~30 nM, respectively. YKL-05-099 has slightly less potent [1] SIK2-inhibitory (IC 50=40 nM) . Purity: 99.76% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

96 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] SPHK Sphingosine kinase

SphK (sphingosine kinase) is the major source of the bioactive lipid and GPCR (G-protein-coupled receptor) agonist S1P (sphingosine 1-phosphate). S1P promotes cell growth, survival and migration, and is a key regulator of lymphocyte trafficking. Inhibition of S1P signalling has been proposed as a strategy for treatment of inflammatory diseases and cancer. S1P is an extracellular ligand at five cognate GPCRs, S1PRs and a consequential intracellular lipid intermediate that affects diverse cellular processes including migration, growth and survival. S1P regulates function and trafficking of immune cells, induces angiogenesis and regulates endothelial cell functions, promotes survival and migration of cancer cells, and has been implicated as an important mediator in the pathogenesis of cancer and autoimmune and allergic diseases.

www.MedChemExpress.com 97 SPHK Inhibitors & Modulators

K145 K145 hydrochloride Cat. No.: HY-15779 Cat. No.: HY-15779A

Bioactivity: K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 Bioactivity: K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM , while no inhibition of SphK1 at concentrations up to 10 μM. IC50 value: 4.3 uM [1] Target: SphK2 in vitro: K145 μM. IC50 value: 4.3 uM [1] Target: SphK2 in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at… with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at… Purity: >98% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

MHP MP-A08 (Methyl caprooyl tyrosinate) Cat. No.: HY-101572 Cat. No.: HY-19794

Bioactivity: MHP is an activator of sphingosine kinase ( SPHK1), and Bioactivity: MP-A08 is a highly selective ATP competitive SK inhibitor that significantly stimulates CAMP mRNA and protein production in targets both SK1 and SK2 with Kivalues of 6.9 ± 0.8 μM and 27 KC. ± 3 μM, respectively.

Purity: 98.02% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 20 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

Opaganib PF-543 (ABC294640) Cat. No.: HY-16015 (Sphingosine Kinase 1 Inhibitor II) Cat. No.: HY-15425

Bioactivity: Opaganib (ABC294640) is a selective, competitive sphingosine Bioactivity: PF-543 is a novel cell-permeant inhibitor of SPHK1 with a Ki kinase 2 ( SK2) inhibitor with K of 9.8 μM. i of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.

Purity: 99.68% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

PF-543 Citrate Phorbol 12-myristate 13-acetate (Sphingosine Kinase 1 Inhibitor II (Citrate)) Cat. No.: HY-15425A (PMA) Cat. No.: HY-18739

Bioactivity: PF-543 Citrate is a novel cell-permeant inhibitor of SPHK1 Bioactivity: Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is an activator of SphK through protein kinase C (PKC) activation. with a Ki of 4.3 nM and more than 100-fold selectivity for SPHK1 over SPHK2.

Purity: 98.22% Purity: 99.08% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 1 mg, 5 mg, 10 mg, 25 mg

SK1-IN-1 SKI II Cat. No.: HY-101805 Cat. No.: HY-13822

Bioactivity: SK1-IN-1 is a potent sphingosine kinase 1 ( SPHK1) inhibitor Bioactivity: SKI-II is an oral active and synthetic inhibitor of sphingosine

with an IC50 of 58 nM. kinase (SK) activity, with IC50 values of 78 μM and 45 μM for SK1 and for SK2, respectively. SKI II causes an irreversible inhibition of SK1 by inducing its lysosomal and/or proteaso…

Purity: 98.0% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 10 mg, 25 mg, 50 mg, 100 mg, 200 mg

98 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] STING Stimulator of Interferon Genes;TMEM173;MITA;ERIS;MPYS

STING (Stimulator of Interferon Genes) is a transmembrane protein localized to the endoplasmic reticulum that undergoes a conformational change in response to direct binding of cyclic dinucleotides (CDNs), resulting in a downstream signaling cascade involving TBK1 activation, IRF-3 phosphorylation, and production of IFN-β and other cytokines. STING is a pattern recognition receptor of cyclic dinucleotides as well as an innate immune adaptor protein that enables signaling from cytoplasmic receptors to the transcription factor interferon regulatory factor 3. Initiation of these pathways leads to the expression of type I interferons and proteins associated with antiviral and antitumor immunity. Small molecules capable of triggering STING-dependent cellular processes are effective at blocking virus replication, enhancing vaccine efficacy, and facilitating immune response to cancer cells.

www.MedChemExpress.com 99 STING Inhibitors & Modulators

ADU-S100 ADU-S100 ammonium salt (ML RR-S2 CDA; MIW815) Cat. No.: HY-12885 (ML RR-S2 CDA (ammonium salt); MIW815 (ammonium salt)) Cat. No.: HY-12885B

Bioactivity: ADU-S100 (ML RR-S2 CDA; MIW815) is an activator of stimulator Bioactivity: ADU-S100 ammonium salt (ML RR-S2 CDA ammonium salt; MIW815 of interferon genes ( STING) [1]. ammonium salt) is an activator of stimulator of interferon genes ( STING).

Purity: 99.23% Purity: 99.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

C-176 CCCP (Carbonyl cyanide 3-chlorophenylhydrazone; Carbonyl Cat. No.: HY-112906 Cyanide m-Chlorophenylhydrazone) Cat. No.: HY-100941

Bioactivity: C-176 is a strong and covalent mouse STING inhibitor. Bioactivity: CCCP is an oxidative phosphorylation uncoupler.

Purity: 98.10% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 50 mg

cGAMP ChX710 (Cyclic AMP-GMP; Cyclic GMP-AMP) Cat. No.: HY-12512 Cat. No.: HY-112951

Bioactivity: cGAMP(Cyclic GMP-AMP) is an endogenous second messenger in Bioactivity: ChX710 could prime the type I interferon response to cytosolic metazoans and triggers interferon production in response to DNA, which induces the ISRE promoter sequence, specific cytosolic DNA; STING ligand. Target: in vitro: cGAMP induced cellular Interferon-Stimulated Genes (ISGs), and the IFNβ RNA robustly even at concentrations as low as 10 nM. phosphorylation of Interferon Regulatory Factor (IRF) 3. cGAMP was much more potent than c-di-GMP in inducing IFNβ… Purity: 98.56% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 500u g, 1 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

CL656 Cyclic-di-GMP (c-[2’FdAMP(S)-2’FdIMP(S)]) Cat. No.: HY-112878 (c-di-GMP; cyclic diguanylate; 5GP-5GP) Cat. No.: HY-107780

Bioactivity: CL656 is an activator of stimulator of interferon genes ( Bioactivity: Cyclic-di-GMP is a STING agonist and a ubiquitous second STING). messenger that regulates biofilm formation, motility, and virulence in diverse bacterial species.

Purity: >98% Purity: 99.26% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 1 mg

diABZI STING agonist-1 diABZI STING agonist-1 Tautomerism Cat. No.: HY-112921A Cat. No.: HY-112921

Bioactivity: diABZI STING agonist-1 is a selective stimulator of interferon Bioactivity: diABZI STING agonist-1 (Tautomerism) is a selective stimulator

genes (STING) receptor agonist. of interferon genes (STING) receptor agonist, with an EC50s of 130 for human PBMCs.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 250 mg, 500 mg

100 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected]

diABZI STING agonist-1 trihydrochloride H-151 Cat. No.: HY-112921B Cat. No.: HY-112693

Bioactivity: diABZI STING agonist-1 (trihydrochloride) is a selective Bioactivity: H-151 is a highly potent, selective and covalent antagonist of stimulator of interferon genes (STING) receptor agonist. STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation [1].

Purity: 99.89% Purity: 97.08% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

STING agonist-1 STING ligand-1 (G10) Cat. No.: HY-19711 Cat. No.: HY-114399

Bioactivity: STING agonist-1 (G10) is a novel human-specific STING agonist Bioactivity: STING ligand-1 is a lead STING ligand with an IC50 of 68 nM for that elicits antiviral activity against emerging Alphaviruses. HAQ STING [1]. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) (IC90 = 24.57 μ…

Purity: 99.06% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 500 mg, 250 mg 5 mg, 10 mg, 50 mg, 100 mg

Vadimezan (ASA-404; DMXAA) Cat. No.: HY-10964

Bioactivity: Vadimezan (ASA-404; DMXAA), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes ( STING) and also a potent inducer of type I IFNs and other cytokines.

Purity: 99.81% Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 101 Thrombopoietin Receptor

Thrombopoietin (TPO) is the major regulator of megakaryocytopoiesis and platelet formation. The protein encoded by the c-mpl gene, CD110, is a 635 amino acid transmembrane domain, with two extracellular cytokine receptor domains and two intracellular cytokine receptor box motifs. Upon binding of thrombopoietin CD110 is dimerized and the JAK family of non-receptor tyrosine kinases, as well as the STAT family, the MAPK family, the adaptor protein Shc and the receptors themselves become tyrosine phosphorylated. TPO binds to the thrombopoietin receptor (TPOr, also termed c-mpl) on platelets, megakaryocytes, and pluripotent stem cells leading to inhibition of apoptosis of stem cells and megakaryocytes; increased megakaryocyte number, size, and ploidy; increased rate of megakaryocyte maturation and platelet count; and decreased platelet threshold for activation by ADP and collagen.

102 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Thrombopoietin Receptor Inhibitors & Modulators

Avatrombopag Eltrombopag (AKR-501; E5501; YM477) Cat. No.: HY-13463 (SB-497115) Cat. No.: HY-15306

Bioactivity: Avatrombopag(AKR-501; AS1670542) is a novel orally-active Bioactivity: Eltrombopag is a thrombopoietin (TPO) receptor agonist thrombopoietin(TPO) receptor agonist with EC50 of 3.3 nM. EC50 developed for certain conditions that lead to value: 3.3 nM [1] Target: TPO receptor agonist in vitro: thrombocytopenia. AKR-501 specifically targeted the TPO receptor and stimulated megakaryocytopoiesis throughout the development and Purity: maturation…97.81% Purity: 98.41% Clinical Data: Phase 3 Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 10 mg, 50 mg, 100 mg

Eltrombopag Olamine Lusutrombopag (Eltrombopag diethanolamine salt; SB-497115GR) Cat. No.: HY-15306A (S-888711) Cat. No.: HY-19883

Bioactivity: Eltrombopag is a thrombopoietin-receptor agonist used to Bioactivity: Lusutrombopag is an orally bioavailable thrombopoietin treat low blood platelet counts with chronic immune (TPO) receptor agonist, used for treatment of chronic liver thrombocytopenia. disease.

Purity: 99.56% Purity: 98.81% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg, 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

TPO agonist 1 Cat. No.: HY-100380

Bioactivity: TPO agonist 1 can increase production of platelets by stimulating the TPO receptor in people with chronic ITP.

Purity: 95.58% Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 103 Toll-like Receptor (TLR)

Toll-like receptors (TLRs) are a class of proteins that play a key role in the innate immune system. They are single, membrane-spanning, non-catalytic receptors usually expressed in sentinel cells such as macrophages and dendritic cells, that recognize structurally conserved molecules derived from microbes. Once these microbes have breached physical barriers such as the skin or intestinal tract mucosa, they are recognized by TLRs, which activate immune cell responses. The TLRs include TLR1, TLR2, TLR3, TLR4, TLR5, TLR6, TLR7, TLR8, TLR9, TLR10, TLR11, TLR12, and TLR13. Toll-Like Receptors (TLRs) play a critical role in the early innate immune response to invading pathogens by sensing microorganism and are involved in sensing endogenous danger signals. TLRs are evolutionarily conserved receptors are homologues of the Drosophila Toll protein, discovered to be important for defense against microbial infection. TLRs recognize highly conserved structural motifs known as pathogen-associated microbial patterns (PAMPs), which are exclusively expressed by microbial pathogens.

104 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Toll-like Receptor (TLR) Inhibitors & Modulators

AN-3485 Atractylenolide I Cat. No.: HY-18325 Cat. No.: HY-N0201

Bioactivity: AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) Bioactivity: Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, inhibitor with IC50 values ranging from 18 to 580 nM. such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and… Purity: >98% Purity: 99.08% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 250 mg, 500 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg

C29 Chloroquine diphosphate Cat. No.: HY-100461 Cat. No.: HY-17589

Bioactivity: C29 is a Toll-like receptor 2 (TLR2) inhibitor. Bioactivity: Chloroquine (diphosphate) is an antimalarial and anti-inflammatory drug widely used to treat malaria and rheumatoid arthritis. Chloroquine is an inhibitor of autophagy and toll-like receptors (TLRs).

Purity: 98.0% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in Water, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg 100 mg

CU-CPT-8m CU-CPT-9a (TLR8-specific antagonist) Cat. No.: HY-112050 Cat. No.: HY-112667

Bioactivity: CU-CPT-8m is a specific TLR8 antagonist, with an IC50 of 67 Bioactivity: CU-CPT-9a is a specific TLR8 antagonist, with an IC50 of 0.5 nM. nM.

Purity: 99.93% Purity: 98.62% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

CU-CPT-9b CU-CPT17e (TLR8-specific antagonist 1) Cat. No.: HY-112051 Cat. No.: HY-101929

Bioactivity: CU-CPT-9b is a specific TLR8 antagonist, with an IC50 of 0.7 Bioactivity: CU-CPT17e is a multi- Toll-like receptor ( TLR) agonist that nM. activates TLR3, TLR8, and TLR9.

Purity: 99.05% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 50 mg, 100 mg

CU-CPT22 Gardiquimod trifluoroacetate Cat. No.: HY-108471 Cat. No.: HY-103697A

Bioactivity: CU-CPT22 is a toll-like receptor 1 and 2 ( TLR1/2) inhibitor Bioactivity: Gardiquimod trifluoroacetate is a specific TLR7 agonist which

with an IC50 of 0.58 µM. can also inhibit HIV-1 reverse transcriptase.

Purity: 99.0% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

www.MedChemExpress.com 105

Hydroxychloroquine sulfate IAXO-102 (HCQ sulfate) Cat. No.: HY-B1370 Cat. No.: HY-125171

Bioactivity: Hydroxychloroquine sulfate is a synthetic antimalarial drug Bioactivity: IAXO-102 is a TLR4 antagonist, inhibits MAPK and p65 NF-kB which can also inhibit Toll-like receptor 7/9 ( TLR7/9) phosphorylation involved in down regulation of the expression signaling. of TLR4 and TLR4 dependent proinflammatory protein. IAXO-102 prevents experimental abdominal aortic aneurysm development [1]. Purity: 99.99% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 500 mg, 250 mg 50 mg

Imiquimod Imiquimod hydrochloride (R 837) Cat. No.: HY-B0180 (R 837 hydrochloride) Cat. No.: HY-B0180A

Bioactivity: Imiquimod (R 837) is an immune response modifier that acts as Bioactivity: Imiquimod hydrochloride is an immune response modifier that a toll-like receptor 7 agonist. acts as a toll-like receptor 7agonist.

Purity: 99.37% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg, 200 mg, 500 mg 100 mg, 200 mg, 500 mg

Imiquimod maleate LHC-165 (R 837 maleate) Cat. No.: HY-B0180B Cat. No.: HY-111786

Bioactivity: Imiquimod maleate is an immune response modifier that acts as Bioactivity: LHC-165 is a TLR7 agonist. Has potential to treat solid a toll-like receptor 7agonist. tumors [1] [2].

Purity: >98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 100 mg, 200 mg, 500 mg Size: 500 mg, 250 mg

MD2-IN-1 MD2-TLR4-IN-1 Cat. No.: HY-103483 Cat. No.: HY-128598

Bioactivity: MD2-IN-1 is an inhibitor of Myeloid differentiation protein Bioactivity: MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid 2 ( MD2) with a KD of 189 μM for the recombinant human differentiation protein 2/toll-like receptor 4 (MD2-TLR4) MD2 ( rhMD2). complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and

interleukin-6 (IL-6) in macrophages with IC50 values of 0.89… Purity: 99.85% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 250 mg, 100 mg, 500 mg 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

MMG-11 Motolimod Cat. No.: HY-112146 (VTX-2337; VTX-378) Cat. No.: HY-13773

Bioactivity: MMG-11 is a potent and selective human TLR2 antagonist. Bioactivity: Motolimod is a selective Toll-like receptor 8 (TLR8) agonist,

MMG-11 inhibits both TLR2/1 and TLR2/6 signaling with an IC with an EC50 of approximately 100 nM. 50 of 1.7 µM for Pam 3CSK 4-induced hTLR2/1 and 5.7 µM for [1] Pam 2CSK 4-induced hTLR2/6 responses . Purity: >98% Purity: 98.83% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 500 mg, 250 mg, 100 mg Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg

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Neoseptin 3 Okanin Cat. No.: HY-U00435 Cat. No.: HY-N6673

Bioactivity: Neoseptin 3 is a Toll-like receptor 4/myeloid differentiation Bioactivity: Okanin, effective constituent of the flower tea Coreopsis

factor 2 ( mTLR4/MD-2) agonist with an EC50 of 18.5 μM. tinctoria, attenuates LPS-induced microglial activation through inhibition of the TLR4/ NF-κB signaling pathways [1].

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg Size:

Paquinimod PF-4878691 (ABR 25757) Cat. No.: HY-100442 (3M-852A) Cat. No.: HY-100176

Bioactivity: Paquinimod is a S100A9 inhibitor, which prevents S100A9 Bioactivity: PF-4878691 is a potent and selective Toll-like receptor 7 ( binding to TLR-4. TLR7) agonist.

Purity: 98.38% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg, 100 mg 1 mg, 5 mg, 10 mg

Procyanidin B1 Resatorvid Cat. No.: HY-N0795 (TAK-242; CLI-095) Cat. No.: HY-11109

Bioactivity: Procyanidin B1 is a polyphenolic flavonoid isolated from Bioactivity: Resatorvid (TAK-242) is a potent TLR4 signaling inhibitor commonly eaten fruits, binds to TLR4/MD-2 complex, and has which selectively inhibits the TLR4-mediated production of anti-inflammatory activity. cytokines and nitric oxide.

Purity: 99.92% Purity: 99.95% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg 5 mg, 10 mg, 50 mg, 100 mg

Resiquimod Schaftoside (R848; S28463) Cat. No.: HY-13740 Cat. No.: HY-N0703

Bioactivity: Resiquimod is a Toll-like receptor 7 and 8 ( TLR7/TLR8) Bioactivity: Schaftoside is a flavonoid found in a variety of Chinese agonist that induces the upregulation of cytokines such as herbal medicines, such as Eleusine indica. Schaftoside inhibits TNF-α, IL-6 and IFN-α. the expression of TLR4 and Myd88. Schaftoside also decreases Drp1 expression and phosphorylation, and reduces mitochondrial fission [1]. Purity: 99.85% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 25 mg, 50 mg, 100 mg

Telratolimod TLR7 agonist 1 (MEDI 9197; 3M 052) Cat. No.: HY-109104 Cat. No.: HY-111358

Bioactivity: Telratolimod is a toll like receptors 7/8 ( TLR7/8) agonist, Bioactivity: TLR7 agonist 1 is a potent, selective and oral TLR7 agonist

with antitumor activity. with an IC50 of 90 nM.

Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 500 mg, 250 mg

www.MedChemExpress.com 107

TLR7 agonist 2 TLR7/8 agonist 1 dihydrochloride Cat. No.: HY-103039 Cat. No.: HY-103698A

Bioactivity: TLR7 agonist 2 is a potent and selective Toll-like Receptor 7 Bioactivity: TLR7/8 agonist 1 dihydrochloride is a toll-like receptor ( ( TLR7) agonist with a LEC of 0.4 μM. TLR7)/ TLR8 dual-agonistic imidazoquinoline.

Purity: 98.82% Purity: 98.02% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Toll-like receptor modulator Vesatolimod Cat. No.: HY-10018 (GS-9620) Cat. No.: HY-15601

Bioactivity: Toll-like receptor modulator is a modulator of TLR7/8, which Bioactivity: Vesatolimod (GS-9620) is a potent, selective and orally active

modulates immune function. agonist of Toll-Like Receptor (TLR7) with an EC50 of 291 nM.

Purity: 99.40% Purity: 99.56% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 50 mg 5 mg, 10 mg, 50 mg, 100 mg

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