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Home , Diprophylline, Istradefylline, Preladenant, Proxyphylline, Rolofylline, Theophylline

Adenosine P1 receptor

Adenosine receptors (ARs) comprise a group of G protein-coupled receptors (GPCR) which mediate the physiological actions of adenosine. To date, four AR subtypes have been cloned and identified in different tissues. These receptors have distinct localization, signal transduction pathways and different means of regulation upon exposure to agonists. A key property of some of Adenosine receptors is their ability to serve as sensors of cellular , which is transmitted by transcription factors, such as NF-κB, to regulate the expression of ARs. The importance of Adenosine receptors in the regulation of normal and pathological processes such as sleep, the development of cancers and in protection against hearing loss will be examined.

www.MedChemExpress.com 1 Inhibitors, Agonists, Antagonists, Activators & Modulators

(Rac)-Mirabegron D5 5'-N-Ethylcarboxamidoadenosine ((Rac)-YM178 D5) Cat. No.: HY-14773S (NECA) Cat. No.: HY-103173

(Rac)-Mirabegron D5 ((Rac)-YM178 D5) is a 5'-N-Ethylcarboxamidoadenosine (NECA) is a deuterium labeled (Rac)-Mirabegron. nonselective adenosine receptor agonist. (Rac)-Mirabegron is the racemate of Mirabegron.

Mirabegron is a selective β3-adrenoceptor agonist.

Purity: >98% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

8-Cyclopentyl-1,3-dimethylxanthine A2A 1 Cat. No.: HY-W011955 (CPI-444 analog) Cat. No.: HY-102024

8-Cyclopentyl-1,3-dimethylxanthine (Compound 2a) A2A receptor antagonist 1 (CPI-444 analog) is an

is a selective antagonist antagonist of both and

with Kis of 10.9 nM and 1440 nM for A1 receptor A1 receptor with Ki values of 4 and 264 nM, and A2 receptor, respectively. respectively.
.

Purity: >98% Purity: 99.81% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

A2AR-agonist-1 A2B receptor antagonist 1 Cat. No.: HY-18776 Cat. No.: HY-U00321

A2AR-agonist-1 is a potent A2AR and ENT1 agonist A2B receptor antagonist 1 is a potent A2B with Ki of 4.39 and 3.47 for A2AR and ENT1. IC50 adenosine receptor antagonist extracted from value: 4.39 and 3.47 (Ki) Target: A2AR and ENT1 patent WO 2009157938 A1 EXAMPLE 9B. A2AR-agonist-1 is a novel dual-action compound, targeting the Adenosine A2A Receptor and Adenosine Transporter for Neuroprotection. Purity: 99.96% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

AB-MECA AB928 Cat. No.: HY-19365 Cat. No.: HY-129393

AB-MECA is a high affinity A3 adenosine receptor AB928 is an orally bioavailable, selective dual agonist, has high affinity for recombinant A1 and adenosine receptor (A2aR/A2bR) antagonist. AB928 A3 receptors. relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.

Purity: 99.10% Purity: 99.30% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Acefylline Adenosine 5'-monophosphate monohydrate (Theophyllineacetic acid; -7-acetic acid) Cat. No.: HY-B1505 (5'-AMP monohydrate) Cat. No.: HY-A0181A

Acefylline (Theophyllineacetic acid), a Adenosine 5'-monophosphate monohydrate is an

derivative, is an adenosine receptor antagonist. adenosine A1 receptor agonist. Adenosine Acefylline is a peptidylarginine deiminase (PAD) 5'-monophosphate monohydrate has significant activator. Acefylline is also a , antiviral activity against HSV-1 and HSV-2. which inhibits rat lung cAMP isoenzymes. Purity: 99.89% Purity: 99.07% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 100 mg Size: 10 mM × 1 mL, 500 mg, 1 g

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

Adenosine A1 receptor activator T62 Adenosine amine congener Cat. No.: HY-106199 (ADAC) Cat. No.: HY-128064

Adenosine A1 receptor activator T62 is an Adenosine amine congener (ADAC) is a selective A1 allosteric enhancer of adenosine A1 receptor. adenosine receptor agonist, can ameliorate noise- Adenosine A1 receptor activator T62 produces and Cisplatin-induced cochlear injury. Adenosine antinociception in animal models of acute pain and amine congener also has neuroprotective effects. also reduces hypersensitivity in models of inflammatory and nerve-injury pain. Purity: ≥98.0% Purity: 99.23% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg Size: 10 mM × 1 mL, 5 mg

Adenosine antagonist-1 Adenosine-2'-monophosphate Cat. No.: HY-100274 (2'-AMP; Adenosine 2'-phosphate; AMP 2'-phosphate) Cat. No.: HY-124151

Adenosine antagonist-1 is an Adenosine-2'-monophosphate (2'-AMP) is converted (AA3R) antagonist. by extracellular 2’,3'-CAMP. Adenosine-2'-monophosphate is further metabolized to extracellular adenosine (a mechanism called the extracellular 2’,3’-cAMP-adenosine pathway).

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

Aminophylline APNEA Cat. No.: HY-B0140 (N6-[2-(4-Aminophenyl)ethyl]adenosine) Cat. No.: HY-18687

Aminophylline is a competitive and non-selective APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a phosphodiesterase (PDE) inhibitor. Aminophylline potent, non-selective A3 adenosine receptor is a competitive adenosine receptor antagonist. agonist. Aminophylline has apulmonary vasodilator action as well as a bronchodilator action and has the potential for research. Purity: 99.91% Purity: 95.01% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

AZD4635 BAY 60-6583 (HTL1071) Cat. No.: HY-101980 Cat. No.: HY-103171

AZD4635 (HTL1071) is a potent, selective and BAY 60-6583 is a potent and high-affinity agonist orally active adenosine A2A receptor (A2AR) of (EC50 = 3 nM) antagonist. AZD4635 binds to human A2AR with a over A1, A2A, and A3 receptors. BAY 60-6583 binds

Ki of 1.7 nM and shows >30-fold selectivity to mouse, rabbit, and dog A2BAR with Ki values of over other adenosine receptors. 750 nM, 340 nM and 330 nM, respectively.

Purity: 99.68% Purity: 99.58% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

BAY-545 Capadenoson Cat. No.: HY-111767 (BAY 68-4986) Cat. No.: HY-14917

BAY-545 is a potent and selective A2B adenosine Capadenoson is a selective agonist of adenosine-A1 receptor antagonist, with an IC50 of 59 nM. receptor.

Purity: 97.06% Purity: 99.28% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

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CGS 15943 CGS 21680 Cat. No.: HY-100678 Cat. No.: HY-13201

CGS 15943 is an orally bioavailable non-xanthine CGS 21680 is a selective adenosine A2A receptor

Adenosine Receptor antagonist. Its Ki for human agonist, with a Ki of 27 nM. A1, A2A, A2B, and A3 Adenosine Receptors are 3.5, 4.2, 16, and 50 nM in transfected CHO cells, respectively.

Purity: 99.63% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg Size: 1 mg, 5 mg

CGS 21680 Hydrochloride Cirazoline hydrochloride Cat. No.: HY-13201A (LD 3098 hydrochloride) Cat. No.: HY-101300

CGS 21680 Hydrochloride is a selective adenosine Cirazoline hydrochloride (LD 3098 hydrochloride)

A2A receptor agonist with a Ki of 27 nM. is a potent competitive full α1A-adrenergic

receptor (α1A-AR) agonist (Ki=120 nM) and only a

partial agonist at α1B-AR (Ki= 960 nM) and α1D-AR

(Ki=660 nM).

Purity: 99.70% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 50 mg

CPI-444 Derenofylline (V81444; ciforadenant) Cat. No.: HY-101978 (SLV 320) Cat. No.: HY-14858

CPI-444 (V81444) is a potent, orally active and Derenofylline (SLV 320) is a potent, selective and

selective adenosine A2A receptor (A2AR) orally active adenosine A1 receptor antagonist,

antagonist, which induces antitumor responses. with Ki values of 1 nM, 200 nM and 398 nM for

human A1, A3 and A2A receptors respectively.

Purity: 99.94% Purity: 98.26% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg

Diphylline () Cat. No.: HY-B0128 Cat. No.: HY-B0004

Diphylline (Diprophylline) is a potent A1/A2 Doxofylline is an antagonist of adenosine A1 adenosine receptor antagonist and cyclic receptor which also inhibits phosphodiesterase IV. phosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator and has the potential for chronic and emphysema. Purity: 99.07% Purity: 99.32% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg

DPCPX FSCPX (PD 116948) Cat. No.: HY-100937 Cat. No.: HY-116042

DPCPX (PD 116948), a xanthine derivative, is a FSCPX is a potent and selective irreversible

highly potent and selective Adenosine A1 receptor antagonist of A1 adenosine receptor (A1AR), 3 antagonist, with a Ki of 0.46 nM in H-CHA with low nanomolar potency for binding to the

binding to A1 receptors in rat whole brain A1AR. membranes.

Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

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

GP531 GR79236 Cat. No.: HY-U00116 Cat. No.: HY-18978

GP531 is a potent, second-generation adenosine GR79236 is a highly potent, selective and orally regulating agent, is pharmacologically silent active adenosine A1 receptor agonist with a Kis of under basal conditions but increases localized 3.1 nM and 1300 nM for A1 and A2 receptors, endogenous adenosine during ischemia. respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.

Purity: 98.95% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

GS-6201 HEMADO (CVT-6883) Cat. No.: HY-10081 Cat. No.: HY-103187

GS-6201 (CVT-6883) is a selective adenosine A2B HEMADO is a potent and selective adenosine A3 receptor antagonist. GS-6201 displays high receptor agonist with a Ki of 1.1 nM at the human affinity and selectivity for the human adenosine A3 subtype.

A2B receptors (Ki=22 nM).

Purity: ≥98.0% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 1 mg, 5 mg

Inosine Cat. No.: HY-N0092 (KW-6002) Cat. No.: HY-10888

Inosine is an endogenous Istradefylline is a very potent, selective and produced by catabolism of adenosine. Inosine has orally active adenosine A2A receptor antagonist anti-inflammatory, antinociceptive, with Ki of 2.2 nM in experimental models of immunomodulatory and neuroprotective effects. Parkinson's disease.

Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors. Purity: ≥98.0% Purity: 99.84% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 1 g, 10 g, 25 g, 100 g Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg

KF21213 KFM19 Cat. No.: HY-U00180 Cat. No.: HY-U00251

KF21213 is a highly selective for mapping KFM19 is a potent, selective Adenosine receptor

CNS adenosine A2A receptors. KF21213 shows a (A1-receptor) antagonist, with an IC50 of 50 nM. high affinity for the adenosine A2A receptors

(Ki=3.0 nM).

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

KI-7 LAS101057 Cat. No.: HY-131032 Cat. No.: HY-14390

KI-7 is an A2B adenosine receptor positive LAS101057 is a potent, selective, and orally . KI-7 potentiates the cAMP efficacious A2B receptor antagonist. accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM).

Purity: >98% Purity: 99.78% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

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LUF6000 MRE3008F20 Cat. No.: HY-13236 Cat. No.: HY-103178

LUF6000 is an orally active allosteric modulator MRE3008F20 is a highly potent and selective of the A3 adenosine receptor. LUF6000 has potent antagonist of adenosine A3 receptor (AA3R), anti-inflammatory effect. inhibiting agonist-induced cAMP elevation in

resting T lymphocytes with an IC50 of 5 nM.

Purity: 99.57% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg

MRS 1523 MRS 1754 Cat. No.: HY-121119 Cat. No.: HY-14121

MRS 1523 is a potent and selective adenosine A3 MRS 1754 is a selective antagonist radioligand for

receptor antagonist with Ki values of 18.9 nM and A2B adenosine receptor with very low affinity

113 nM for human and rat A3 receptors, for A1 and A3 receptors of both humans and rats. respectively. In rat this corresponds to

selectivities of 140- and 18-fold vs A1 and A2A receptors, respectively. Purity: >98% Purity: 98.31% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg

MRS-1191 MRS-1706 Cat. No.: HY-124543 Cat. No.: HY-103186

MRS-1191 is a potent and selective A3 adenosine MRS-1706 is a potent and selective adenosine A2B

receptor antagonist with a KB value of 92 nM, receptor inverse agonist. MRS-1706 has Ki values

a Ki value of 31.4 nM for human A3 receptor and of 1.39, 112, 157, and 230 nM for human A2B,

an IC50 of 120 nM for CHO cells. A2A, A1 and A3 receptors respectively.

Purity: 98.57% Purity: 98.06% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

MRS-3777 hemioxalate MRS1177 Cat. No.: HY-110037 Cat. No.: HY-120090

MRS-3777 hemioxalate is a selective adenosine A3 MRS1177 is a potent and selective human Adenosine

receptor antagonist. A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.

Purity: 95.64% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 1 mg, 5 mg

MRS1186 N-0861 racemate Cat. No.: HY-118678 Cat. No.: HY-U00143

MRS1186 is a potent and selective human Adenosine N-0861 racemate is the racemate of N-0861. N-0861

A3 receptor (hA3AR) antagonist, with a Ki of is a selective adenosine A1 receptor antagonist. 7.66 nM.

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

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

N-[(4-Aminophenyl)methyl]adenosine N6-(2-Phenylethyl)adenosine Cat. No.: HY-100130 (N6-Phenethyladenosine; N6-Phenylethyladenosine) Cat. No.: HY-101854

N-[(4-Aminophenyl)methyl]adenosine is a adenosine N6-(2-Phenylethyl)adenosine receptor inhibitor, with Ki of 29 nM for Rat (N6-Phenethyladenosine), an adenosine derivative, ecto-5′-Nucleotidase. IC50 value: 29.0 ± 1.7 nM is a potent adenosine receptors (AR) agonist with

(Ki) Target: Adenosine Receptor. Ki values of 11.8 nM, 30.1 nM, 0.63 nM for rat

A1AR, human A1AR and hA3AR, respectively.

Purity: 98.68% Purity: 99.86% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg, 200 mg

N6-Cyclohexyladenosine N6-Cyclopentyladenosine (CHA) Cat. No.: HY-18939 (CPA; UK-80882) Cat. No.: HY-103181

N6-Cyclohexyladenosine is a selective A1 receptor N6-Cyclopentyladenosine (CPA) is a selective agonist (EC50 = 8.2 nM). Adenosine A1 receptor agonist, with Ki values of

2.3 nM, 790 nM and 43 nM for human A1, A2A and

A3 receptors, respectively.

Purity: 99.98% Purity: 98.72% Clinical Data: No Development Reported Clinical Data: Phase 1 Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

N6-Ethyladenosine Namodenoson Cat. No.: HY-111809 (CF-102; 2-Cl-IB-MECA) Cat. No.: HY-12365

N6-Ethyladenosine is an adenosine derivative, acts Namodenoson (CF-102) is a selective A3 adenosine as a Adenosine receptor agonist, with Kis of 4.9 receptor (A3AR) agonist (Ki=0.33 nM). and 4.7 nM for hA1AR and hA3AR, respectively. Namodenoson displays 2500- and 1400-fold selectivity over A1 and A2A receptors respectively.

Purity: 99.90% Purity: 99.71% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Nitrobenzylthioinosine PD 117519 (NBMPR) Cat. No.: HY-W010936 (CI947) Cat. No.: HY-100032

Nitrobenzylthioinosine is an ENT1 transporter PD 117519 (CI947) is an A2A adenosine agonist inhibitor that binds to ENT1 transporter with which has shown oral antihypertensive activity in high affinity. Nitrobenzylthioinosine is a pharmacological animal models. photoaffinity probe for adenosine uptake sites in brain. Nitrobenzylthioinosine can cross the blood-brain barrier. Purity: ≥98.0% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Piclidenoson (IB-MECA; CF-101) Cat. No.: HY-13591 (SCH-420814) Cat. No.: HY-10889

Piclidenoson (IB-MECA) is a first-in-class, orally Preladenant is a potent and competitive antagonist active and selective A3 adenosine receptor of the human adenosine A2A receptor with a Ki of (A3AR) agonist. Piclidenoson exhibits 1.1 nM and has over 1000-fold selectivity over antiproliferative effect and induces apoptosis in other adenosine receptors. different cancer cell types like melanoma, leukemia. Purity: 99.32% Purity: 99.28% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 5 mg, 10 mg, 50 mg, 100 mg

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Proxyphylline PSB 0777 ammonium Cat. No.: HY-B1742 Cat. No.: HY-136233

Proxyphylline is a methylxanthine derivative used PSB 0777 ammonium is a potent and selective

as a cardiac , vasodilator and adenosine A2A receptor full agonist with Ki

bronchodilator. values of 44.4 nM, 360 nM for rat and human A2A

receptors, respectively. PSB 0777 ammonium has Ki

values of ≥10000 nM, 541 nM for rat and human A1 receptors, respectively. Purity: 98.81% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg Size: 1 mg, 5 mg

Regadenoson (CVT-3146) Cat. No.: HY-A0168 (KW-3902) Cat. No.: HY-10965

Regadenoson (CVT-3146) is a potent and selective Rolofylline (KW-3902) is a potent, selective

A2A adenosine receptor agonist, with Kis of 290 adenosine A1 receptor antagonist that is under and 1120 nM for rat and pig adenosine A2A development for the treatment of patients with receptor, respectively. acute congestive heart failure and renal impairment.

Purity: 99.59% Purity: >98% Clinical Data: Launched Clinical Data: Phase 3 Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg Size: 1 mg, 5 mg

SCH 58261 Sch412348 Cat. No.: HY-19533 Cat. No.: HY-U00189

SCH 58261 is a potent, selective and competitive Sch412348 is a potent competitive antagonist of

antagonist of adenosine A2A receptor with an IC50 the human adenosine A2A receptor (Ki=0.6 nM) and of 15 nM, and displays 323-, 53- and 100-fold more has >1000-fold selectivity over all other selective for A2A receptor than A1, A2B, and A3 adenosine receptors. receptors, respectively.

Purity: 99.71% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

SCH442416 ST3932 Cat. No.: HY-103169 Cat. No.: HY-112840

SCH442416 is a potent, selective and ST3932 is a metabolite of ST1535, acts as an

brain-penetrant antagonist of adenosine A2A antagonist of adenosine A2A receptor, with Kis of

receptor (A2AR), with Kis of 0.048 and 0.5 nM 8 nM and 33 nM for A2A and A1 receptors,

for human and rat A2AR respectively. respectively.

Purity: 98.19% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

ST4206 Swertisin Cat. No.: HY-U00341 Cat. No.: HY-N2189

ST4206 is a potent and orally active adenosine A2A Swertisin, a C-glucosylflavone isolated from

receptor antagonist, with Kis of 12 nM and 197 nM Swertia japonica, is known to have antidiabetic, for adenosine A2A receptor and adenosine A1 anti-inflammatory and effects. receptor, respectively. ST4206 has the potential Swertisin is an adenosine A1 receptor antagonist. for Parkinsons disease research.

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

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

Taminadenant TC-G 1004 Cat. No.: HY-109139 Cat. No.: HY-14365

Taminadenant is an antagonist of adenosine TC-G 1004 (compound 16j) is an orally active A2A receptor. adenosine receptor antagonist, with Ki values of

0.44 nM and 80 nM for hA2A and hA1, respectively.

Purity: 99.43% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Tecadenoson (CVT-510) Cat. No.: HY-19661 (3,7-Dimethylxanthine) Cat. No.: HY-N0138

Tecadenoson (CVT-510) is a selective A1 adenosine Theobromine is a methylxanthine found in cacao receptor agonist. beans which can inhibit adenosine receptor A1 (AR1) signaling.

Purity: 99.76% Purity: 99.74% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 100 mg

Theophylline hydrochloride (1,3-Dimethylxanthine; Theo-24) Cat. No.: HY-B0809 Cat. No.: HY-B0153A

Theophylline is a nonselective phosphodiesterase Ticlopidine hydrochloride is an adenosine (PDE) inhibitor, adenosine receptor blocker, and diphosphate (ADP) receptor inhibitor against histone deacetylase (HDAC) activator. platelet aggregation with IC50 of ~2 μM. Target: (ADP) Ticlopidine (trade name Ticlid) is an antiplatelet drug in the thienopyridine family. Purity: 99.94% Purity: 99.99% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 500 mg, 5 g Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g

Tonapofylline Tozadenant (BG 9928) Cat. No.: HY-14873 (SYN115) Cat. No.: HY-10995

Tonapofylline (BG 9928) is an orally active and Tozadenant is an adenosine A2A receptor selective adenosine A1 receptor antagonist with a antagonist, with Ki of 11.5 nM on human A2A and 6

Ki of 7.4 nM for human adenosine A1 receptor nM on rhesus A2A.

(hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B… Purity: ≥98.0% Purity: 98.65% Clinical Data: Phase 3 Clinical Data: Phase 3 Size: 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Trabodenoson UP202-56 (INO-8875) Cat. No.: HY-106007 Cat. No.: HY-U00226

Trabodenoson (INO-8875), an adenosine mimetic, is UP202-56 is an adenosine analogue, which is an a highly selective Adenosine A1 receptor agonist. agonist. Trabodenoson (INO-8875) is used in the study for Primary Open-Angle Glaucoma.
.

Purity: 98.14% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg

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Vipadenant Xanthine amine congener dihydrochloride (BIIB-014; CEB-4520) Cat. No.: HY-10857 (XAC dihydrochloride) Cat. No.: HY-110303

Vipadenant (BIIB-014; CEB-4520) is an adenosine Xanthine amine congener dihydrochloride (XAC

receptor antagonist, with Kis of 1.3 nM and 68 nM dihydrochloride) is a potent Adenosine A1 receptor

for A2A and A1, respectively. and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.

Purity: 98.02% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

ZM241385 Cat. No.: HY-19532

ZM241385 is a potent, high affinity and selective

adenosine A2a receptor (A2AR) antagonist with

a Ki value of 1.4 nM.

Purity: 99.26% Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

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