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Phosphodiesterase (PDE)

Phosphodiesterase (PDE) is any that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic , which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including C and D, , sphingomyelin phosphodiesterase, DNases, RNases, and restriction , as well as numerous less-well-characterized small- phosphodiesterases. The phosphodiesterases comprise a group of that degrade the phosphodiester bond in the second messenger cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules.

www.MedChemExpress.com 1 Phosphodiesterase (PDE) Inhibitors, Activators & Modulators

(+)-Medioresinol Di-O-β-D-glucopyranoside (R)-(-)- Cat. No.: HY-N8209 ((R)-Rolipram; (-)-Rolipram) Cat. No.: HY-16900A

(+)-Medioresinol Di-O-β-D-glucopyranoside is a (R)-(-)-Rolipram is the R-enantiomer of Rolipram. lignan with strong inhibitory activity Rolipram is a selective inhibitor of

of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM phosphodiesterase. and 240 nM for PDE4A, PDE4B, and PDE4D, respectively.

Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

(R)-DNMDP (S)-(+)-Rolipram Cat. No.: HY-122751 ((+)-Rolipram; (S)-Rolipram) Cat. No.: HY-B0392

(R)-DNMDP is a potent and selective cancer (S)-(+)-Rolipram ((+)-Rolipram) is a cyclic cytotoxic agent. (R)-DNMDP, the R-form of DNMDP, AMP(cAMP)-specific phosphodiesterase (PDE)

binds PDE3A directly. DNMDP binding to PDE3A inhibitor, with an IC50 of 1100 nM. promotes an interaction between PDE3A and Schlafen (S)-(+)-Rolipram can suppresse tumor necrosis 12 (SLFN12). factor-alpha (TNFα) production by human mononuclear cells. Purity: >98% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

3-O-Methylquercetin Cat. No.: HY-N1860 (Theophyllineacetic acid; -7-acetic acid) Cat. No.: HY-B1505

3-O-Methylquercetin (3-MQ), a main constituent of Acefylline (Theophyllineacetic acid), a Rhamnus nakaharai, inhibits total cAMP and derivative, is an antagonist. cGMP-phosphodiesterase (PDE) of guinea pig Acefylline is a peptidylarginine deiminase (PAD) trachealis. 3-O-Methylquercetin (3-MQ) exhibits activator. Acefylline is also a ,

IC50 values of 31.9 μM 86.9 μM 18.6 μM and 1.6 μM which inhibits cAMP phosphodiesterase for PDE1, PDE5, PDE2 and PDE4, respectively. isoenzymes. Purity: >98% Purity: 99.89% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

Acetildenafil AMG 579 Cat. No.: HY-13927 Cat. No.: HY-12913

Acetildenafil is a derivative of the AMG 579 is a potent, selective, and efficacious phosphodiesterase 5 (PDE5) inhibitor . inhibitor of phosphodiesterase 10A (PDE10A) with

an IC50 of 0.1 nM.

Purity: >98% Purity: 99.79% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Amino Cat. No.: HY-117109 Cat. No.: HY-B0140

Amino Tadalafil is an analog of Tadalafil. Aminophylline is a competitive and non-selective Tadalafil is a potent inhibitor of phosphodiesterase (PDE) inhibitor. Aminophylline phosphodiesterase 5 (PDE5) with applications in is a competitive antagonist. several conditions, including erectile Aminophylline has apulmonary vasodilator action as dysfunction, pulmonary arterial , and well as a bronchodilator action and has the lower urinary tract dysfunction. potential for research. Purity: >98% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

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Amrinone AN3199 (Inamrinone) Cat. No.: HY-B1294 Cat. No.: HY-19830

Amrinone (Inamrinone) is a positive AN3199 is a PDE4 inhibitor with an IC50 of 94.5 inotropic-vasodilator agent. Amrinone is a nM. AN3199 can be used for the research of selective phosphodiesterase III inhibitor that -associated diseases such as asthma increases cyclic by and chronic obstructive pulmonary disease (COPD). preventing its breakdown.

Purity: ≥98.0% Purity: 99.67% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Anagrelide hydrochloride (BL4162A) Cat. No.: HY-B0523A (CC-10004) Cat. No.: HY-12085

Anagrelide hydrochloride (BL4162A) is a used Apremilast (CC-10004) is an orally available for the treatment of essential thrombocytosis. inhibitor of type-4 cyclic nucleotide

phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by

lipopolysaccharide (LPS) with an IC50 of 104 nM.

Purity: 99.65% Purity: 99.87% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Apremilast D5 ATX inhibitor 1 (CC-10004 D5) Cat. No.: HY-12085S Cat. No.: HY-111410

Apremilast D5 (CC-10004 D5) is a deuterium labeled ATX inhibitor 1 is a potent ATX (IC50=1.23 nM, Apremilast. Apremilast is an orally available FS-3 and 2.18 nM, bis-pNPP) inhibitor. inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM. Purity: >98% Purity: 99.75% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

ATX inhibitor 5 Autotaxin modulator 1 Cat. No.: HY-133019 Cat. No.: HY-12812

ATX inhibitor 5 is a potent and orally active Autotaxin modulator 1 is an autotaxin (ATX) enzyme autotaxin (ATX) inhibitor, with an IC50 of 15.3 inhibitor, extracted from patent WO 2014018881 A1, nM. ATX inhibitor 5 shows anti-hepatofibrosis Compound Example 12b. effects and reduces CCl4-induced hepatic fibrosis level prominently.

Purity: 99.77% Purity: 98.93% 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

Autotaxin-IN-1 Autotaxin-IN-3 Cat. No.: HY-123637 Cat. No.: HY-135053

Autotaxin-IN-1 is a potent autotaxin inhibitor, Autotaxin-IN-3 is a Autotaxin(ATX) inhibitor with which has favorable potency (IC50=2.2 nM), PK an IC50 of 2.4 nM, compound 33, sourced from properties, and a robust PK/PD relationship. patent WO2018212534A1. Autotaxin-IN-1 is used in treatment of osteoarthritis pain.

Purity: >98% Purity: 98.21% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

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Autotaxin-IN-4 Autotaxin-IN-5 Cat. No.: HY-135088 Cat. No.: HY-135089

Autotaxin-IN-4 (compound 51), extracted from Autotaxin-IN-5 (compound 63), extracted from patent WO2018212534A1, is an Autotaxin inhibitor. patent WO2018212534A1, is an Autotaxin inhibitor. Autotaxin-IN-4 has the potential to treat Autotaxin-IN-5 has the potential to treat idiopathic pulmonary fibrosis. idiopathic pulmonary fibrosis.

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

Avanafil (TA1790) Cat. No.: HY-18252 Cat. No.: HY-N2913

Avanafil(TA-1790) is a potent and highly selective Ayanin is a bioflavonoid isolated from Croton phosphodiesterase-5(PDE-5) inhibitor(IC50=5.2 nM) schiedeanus Schlecht. Ayanin is a non-selective

for ; lower selectivity phosphodiesterase1-4 inhibitor and can be used for against PDE1, PDE6, and PDE11. the study of respiratory disease,such as allergic asthma et al.

Purity: 98.01% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg, 500 mg Size: 1 mg, 5 mg

Balipodect Bay 60-7550 (TAK-063) Cat. No.: HY-12472 (BAY 607550) Cat. No.: HY-14992

Balipodect (TAK-063) is a highly potent, selective Bay 60-7550 is a potent and selective PDE2

and orally active PDE10A inhibitor with IC50 of inhibitor with a Ki of 3.8 nM. 0.30 nM; >15000-fold selectivity over other PDEs.

Purity: 98.69% Purity: 98.12% 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, 100 mg

BAY 73-6691 BAY 73-6691 racemate ((R)-BAY 73-6691) Cat. No.: HY-104028 Cat. No.: HY-104028A

BAY 73-6691 ((R)-BAY 73-6691) is a potent, BAY 73-6691 racemate is a phosphodiesterase 9 penetrant, and selective PDE9A inhibitor. inhibitor extracted from patent WO 2017070293 A1.

Purity: 99.81% Purity: 99.84% 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

BC11-38 BI-2545 Cat. No.: HY-108618 Cat. No.: HY-124772

BC11-38 is a potent, selective, and biologically BI-2545 is a potent autotaxin (ATX) inhibitor that

active PDE11 inhibitor, with IC50s of 0.28 µM and significantly reduces LPA, with IC50s of 2.2 nM >100 µM for PDE11 and PDE1-10, respectively. and 3.4 nM for human ATX and rat ATX, BC11-38 elevates cAMP levels, PKA-mediated ATF-1 respectively. , and cortisol production in H295R cells. Purity: ≥98.0% Purity: 99.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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BI-409306 BIO-32546 Cat. No.: HY-112831 Cat. No.: HY-103035

BI-409306 is a potent and selective PDE9A BIO-32546 (example 12b, S-isomer) is an autotaxin inhibitor, with an IC50 of 52 nM, and shows weak (ATX) modulator, extracted from the patent activity against other PDEs, such as PDE1A (IC50, US20170158687A1.

1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A,

PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the… Purity: 99.46% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg Size: 1 mg, 5 mg

BPN14770 BRD9500 Cat. No.: HY-117571 Cat. No.: HY-136350

BPN14770 is a selective phosphodiesterase 4D BRD9500 is an orally active phosphodiesterases 3

(PDE4D) allosteric inhibitor with IC50s of 7.8 nM (PDE3) inhibitor with IC50s of 10 and 27 nM for and 7.4 nM for PDE4D7 and PDE4D3, respectively. PDE3A and PDE3B, respectively. Antitumor activity.

Purity: 99.39% Purity: 99.60% 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

BRL-50481 Cat. No.: HY-109586 (Dibutyryl cAMP calcium salt; DBcAMP calcium salt) Cat. No.: HY-B0764A

BRL-50481 is a novel and selective inhibitor of Bucladesine calcium salt (Dibutyryl-cAMP calcium

PDE7 with IC50s of 0.15, 12.1, 62 and 490 μM for salt;DC2797 calcium salt) is a cell-permeable PDE7A, PDE7B, PDE4 and PDE3, respectively. cyclic AMP (cAMP) analog and selectively activates cAMP dependent kinase (PKA) by increasing the intracellular level of cAMP.

Purity: 99.90% Purity: 95.73% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 50 mg, 100 mg

Bucladesine sodium Butein (Dibutyryl cAMP sodium salt; DBcAMP sodium salt) Cat. No.: HY-B0764 (2’,3,4,4’-tetrahydroxy Chalcone) Cat. No.: HY-16558

Bucladesine sodium salt (Dibutyryl-cAMP sodium Butein, isolated from Dalbergia odorifera T. Chen, salt) is a stabilized cyclic AMP (cAMP) analog and is a cAMP-specific PDE inhibitor with an IC50 of a selective PKA activator. Bucladesine sodium 10.4 μM for PDE4. Butein is a specific protein salt raises the intracellular levels of cAMP. tyrosine kinase inhibitor with IC50s of 16 and 65 Bucladesine sodium salt is also a phosphodiesterase μM for EGFR and p60c-src in HepG2 cells. (PDE) inhibitor. Purity: 99.71% Purity: 99.95% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mg

BW-A 78U CALP1 Cat. No.: HY-100118 Cat. No.: HY-P1077

BW-A 78U is a PDE4 inhibitor with an IC50 of 3 CALP1 is a (CaM) (Kd of μM. 88 µM) with binding to the CaM EF-hand/Ca2+-. CALP1 blocks calcium

influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening.

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

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CALP1 TFA CALP2 Cat. No.: HY-P1077A Cat. No.: HY-P1076

CALP1 TFA is a calmodulin (CaM) agonist CALP2 is a calmodulin (CaM) antagonist (

(Kd of 88 µM) with binding to the CaM (Kd of 7.9 µM)) with high affinity for binding EF-hand/Ca2+-binding site. CALP1 TFA blocks calcium to the CaM EF-hand/Ca2+-binding site. CALP2

influx and apoptosis (IC50 of 44.78 µM) through inhibits CaM-dependent phosphodiesterase inhibition of calcium channel opening. activity and increases intracellular Ca2+ concentrations. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

CALP2 TFA CDC801 Cat. No.: HY-P1076A Cat. No.: HY-U00179

CALP2 TFA is a calmodulin (CaM) antagonist CDC801 is a potent and orally active

(Kd of 7.9 µM) with high affinity for binding to phosphodiesterase 4 (PDE4) and tumor necrosis 2+ the CaM EF-hand/Ca -binding site. CALP2 TFA factor-α (TNF-α) inhibitor with IC50 of 1.1 μM inhibits CaM-dependent phosphodiesterase and 2.5 μM, respectively. activity and increases intracellular Ca2+ concentrations. Purity: 98.48% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg Size: 1 mg, 5 mg

CI-1044 (PD-189659) Cat. No.: HY-100246 (SB-207499) Cat. No.: HY-10790

CI-1044 is an orally active PDE4 inhibitor with Cilomilast (SB-207499) is a potent, selective and

IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, orally active inhibitor of Phosphodiesterase 4

PDE4B2, PDE4C2 and PDE4D3, respectively. (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively.

Purity: 98.0% Purity: 99.11% Clinical Data: No Development Reported Clinical Data: Phase 3 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

Cilostamide (OPC3689) Cat. No.: HY-101312 (OPC 13013) Cat. No.: HY-17464

Cilostamide is a selective and potent PDE3 Cilostazol (OPC 13013) is a potent and selective

inhibitor, with IC50s of 27 nM and 50 nM for PDE3A inhibitor of phosphodiesterase (PDE) 3A, the and PDE3B, respectively, and has antithrombotic isoform of PDE 3 in the cardiovascular system,

and anti-intimal hyperplastic activity. with an IC50 of 0.2 μM.

Purity: 98.24% Purity: 99.91% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 50 mg, 100 mg

Cirsimarin CM-675 Cat. No.: HY-N7272 Cat. No.: HY-114303

Cirsimarin is a potent antilipogenic CM-675 is a dual phosphodiesterase 5 (PDE5) and isolated from Microtea debilis. Cirsimarin class I histone deacetylases-selective inhibitor,

exerts potent antilipogenic effect and decreases with IC50 values of 114 nM and 673 nM for PDE5 and adipose deposition in mice. HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease.

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]

CP671305 Cat. No.: HY-101803 (AN-2728; PF-06930164) Cat. No.: HY-10978

CP671305 is a potent, orally active, selective Crisaborole (AN-2728) is a potent inhibitor of inhibitor of phosphodiesterase-4-D, and possesses PDE4 and cytokine release; inhibit PDE4 with an high activities. IC50 of 0.49 μM.

Purity: 99.95% Purity: 96.55% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

D159687 Deltarasin Cat. No.: HY-15444 Cat. No.: HY-15747

D159687 is a selective PDE4D inhibitor. Deltarasin is an inhibitor of KRAS-PDEδ

interaction with Kd of 38 nM for binding to purified PDEδ.

Purity: 98.0% Purity: 96.32% 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, 5 mg, 10 mg, 50 mg, 100 mg

Deltarasin hydrochloride Deltasonamide 1 Cat. No.: HY-15747A Cat. No.: HY-122641

Deltarasin hydrochloride is an inhibitor Deltasonamide 1 is a PDE6δ-KRas inhibitor, with a of KRAS-PDEδinteraction KD of 203 pM. with Kd of 38 nM for binding to purified PDEδ.

Purity: 99.97% 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

Deltasonamide 2 Deltasonamide 2 (TFA) Cat. No.: HY-122641A Cat. No.: HY-122641B

Deltasonamide 2 is a competitive, high affinity Deltasonamide 2 TFA is competitive, high affinity

PDEδ inhibitor with a Kd of ~385 pM. PDEδ inhibitor with a Kd of ~385 pM.

Purity: >98% Purity: 99.65% 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, 5 mg, 10 mg, 50 mg, 100 mg

Deltasonamide 2 hydrochloride Difamilast Cat. No.: HY-122641C (OPA-15406) Cat. No.: HY-109085

Deltasonamide 2 hydrochloride is a competitive, Difamilast (OPA-15406) is a topical, selective and high affinity PDEδ inhibitor with a Kd of ~385 nonsteroidal phosphodiesterase-4 (PDE4) inhibitor pM. with particularly efficient inhibition of subtype

B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate (AD). Purity: 99.12% Purity: 99.20% 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, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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Diphylline () Cat. No.: HY-B0128 Cat. No.: HY-B0312

Diphylline (Diprophylline) is a potent A1/A2 Dipyridamole (Persantine) is a phosphodiesterase adenosine receptor antagonist and cyclic inhibitor that blocks uptake and metabolism of nucleotide phosphodiesterase inhibitor. Diphylline, adenosine by erythrocytes and vascular endothelial a xanthine derivative, is a bronchodilator and cells. vasodilator drug and has the potential for chronic bronchitis and emphysema. Purity: 99.07% Purity: 99.70% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg, 500 mg

DNMDP Cat. No.: HY-W028690 Cat. No.: HY-B0004

DNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, Doxofylline is an antagonist of adenosine A1 is a potent and selective cancer cell cytotoxic receptor which also inhibits phosphodiesterase IV. agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity. Purity: 98.95% Purity: 99.32% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 10 mM × 1 mL, 100 mg

DSR-141562 EHNA hydrochloride Cat. No.: HY-136569 Cat. No.: HY-103160A

DSR-141562 is a novel, orally active, and EHNA hydrochloride is a potent and selective dual selective brain-penetrant phosphodiesterase 1 inhibitor of cyclic nucleotide

(PDE1) inhibitor. DSR-141562 shows preferential (PDE2)(IC50=4 μM) and (ADA).

selectivity for human PDE1B with an IC50 of 43.9

nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. Purity: 98.17% 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: 10 mM × 1 mL, 2 mg, 5 mg

Enoximone ent-Tadalafil Cat. No.: HY-B1639 (ent-IC-351) Cat. No.: HY-90009C

Enoximone is an inotropic vasodilating agent and a ent-Tadalafil (ent-IC-351), compound (6S,12aS), is selective and orally active phosphodiesterase III a inactive cis-enantiomer of compound (6R,12aS).

(PDE3) inhibitor with an IC50 of 5.9 μM. compound (6R,12aS) is a potent PDE5 inhibitor

Enoximone induces vasodilatation and increases with an IC50 of 0.090 μM, while ent-Tadalafil is intracellular levels of cAMP by inhibiting inactive at concentrations up to 10 µM. cGMP-inhibited PDE. Purity: 98.05% Purity: 98.14% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

ER21355 FCPR03 Cat. No.: HY-101826 Cat. No.: HY-117977

ER21355 is an inhibitor of phosphodiesterase 5 FCPR03 is a potent and selective phosphodiesterase

(PDE5), used for treatment of prostatic diseases. 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). 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]

Fraxin Furamidine (Fraxoside) Cat. No.: HY-N0579 (DB75; NSC 305831) Cat. No.: HY-110137A

Fraxin isolated from Acer tegmentosum, F. ornus or Furamidine (DB75) is a selective protein A. hippocastanum, is a glucoside of fraxetin and methyltransferase 1 (PRMT1) inhibitor with an reported to exert potent anti-oxidative stress IC50 of 9.4 μM. Furamidine is selective for action, anti-inflammatory and antimetastatic PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) properties. (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Purity: 99.83% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg

Furamidine dihydrochloride Gisadenafil (DB75 dihydrochloride; NSC 305831 dihydrochloride) Cat. No.: HY-110137 (UK-369003) Cat. No.: HY-14841

Furamidine dihydrochloride (DB75 dihydrochloride) Gisadenafil (UK-369003) is a specific, orally is a selective protein arginine methyltransferase 1 active phosphodiesterase 5 (PDE5) inhibitor with

(PRMT1) inhibitor with an IC50 of 9.4 μM. an IC50 of 3.6 nM and prevents degradation of cyclic monophosphate (cGMP).

Purity: ≥98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg Size: 1 mg, 5 mg

Gisadenafil besylate (UK 369003-26) Cat. No.: HY-108619 (O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396) Cat. No.: HY-N3945

Gisadenafil besylate (UK 369003-26) is a specific, Glaucine (O,O-Dimethylisoboldine) is an alkaloid orally active phosphodiesterase 5 (PDE5) inhibitor isolated from Glaucium flavum Crantz with with an IC50 of 3.6 nM and prevents degradation of antitussive, bronchodilation and anti-inflammatory cyclic (cGMP). properties.

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

GSK256066 GSK256066 Trifluoroacetate Cat. No.: HY-10469 Cat. No.: HY-70069

GSK256066 is a selective and high-affinity GSK256066 Trifluoroacetate is a selective and phosphodiesterase 4 (PDE4) inhibitor, with an IC50 high-affinity phosphodiesterase 4 (PDE) inhibitor, of 3.2 pM for PDE4B. GSK256066 is developed for with an IC50 of 3.2 pM for PDE4B. GSK256066 the research of chronic obstructive pulmonary Trifluoroacetate is developed for the research of disease. chronic obstructive pulmonary disease.

Purity: 98.83% Purity: 99.54% Clinical Data: Phase 2 Clinical Data: Phase 2 Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

GSK356278 HA130 Cat. No.: HY-106003 Cat. No.: HY-19329

GSK356278 is a potent, selective, orally HA130 is a selective autotaxin (ATX) inhibitor bioavailable and brain-penetrant inhibitor of with an IC50 of 28 nM. phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively.

Purity: ≥98.0% Purity: 99.43% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

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HA155 Homo Sildenafil Cat. No.: HY-116100A Cat. No.: HY-131100

HA-155 is a potent and selective autotaxin (ATX) Homo Sildenafil, an analog of Sildenafil, acts as

inhibitor with an IC50 of 5.7 nM. a phosphodiesterase inhibitor.

Purity: ≥98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg Size: 1 mg, 5 mg

IBMX (3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine) Cat. No.: HY-12318 (KC-404; AV-411; MN-166) Cat. No.: HY-B0763

IBMX is a broad-spectrum phosphodiesterase (PDE) Ibudilast (KC-404; AV-411; MN-166) is a relatively

inhibitor, with IC50s of 6.5, 26.3 and 31.7 μM for nonselective phosphodiesterase inhibitor which has PDE3, PDE4 and PDE5, respectively. been marketed for treating asthma.

Purity: 99.99% Purity: 99.93% Clinical Data: No Development Reported Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Icariin ICI 153110 (Ieariline) Cat. No.: HY-N0014 Cat. No.: HY-100239

Icariin is a flavonol . Icariin inhibits ICI 153110 is an orally active phosphodiesterase

PDE5 and PDE4 activities with IC50s of 432 nM inhibitor with both vasodilating and inotropic and 73.50 μM, respectively. Icariin also is a properties which is designed for the treatment of PPARα activator. congestive cardiac failure.

Purity: 98.75% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg

Ilexsaponin B2 Cat. No.: HY-N6256 (Dicloguamine) Cat. No.: HY-B0327

Ilexsaponin B2 is a saponin isolated from the root Irsogladine is a PDE4 inhibitor and muscarinic of Ilex pubescens Hook. et Arn. Ilexsaponin B2 is a acetylcholine receptor binder. potent phosphodiesterase 5 (PDE5) and PDEI

inhibitor with IC50 values of 48.8 μM and 477.5 μM, respectively.

Purity: >98% Purity: 99.80% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg

Irsogladine maleate ITI-214 (Dicloguamine maleate; MN1695) Cat. No.: HY-B0327A Cat. No.: HY-12501A

Irsogladine is a PDE4 inhibitor and muscarinic ITI-214 is a potent, CNS-active, orally

acetylcholine receptor binder. bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels.

Purity: >98% Purity: 99.57% Clinical Data: Launched Clinical Data: Phase 2 Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

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

ITI-214 free base K-Ras-PDEδ-IN-1 Cat. No.: HY-12501 Cat. No.: HY-115555

ITI-214 free base is a potent, CNS-active, orally K-Ras-PDEδ-IN-1 is a novel and potent competitive bioavailable PDE1 inhibitor (Ki of 58 pM) with K-Ras-PDEδ inhibitor. K-Ras-PDEδ-IN-1 binds to excellent selectivity against other PDE family the farnesyl binding pocket of PDEδ with a low members and against a panel of enzymes, receptors, nanomolar Kd of 8 nM. transporters and ion channels.

Purity: ≥98.0% Purity: 99.33% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

K134 Kuraridine (OPC33509) Cat. No.: HY-U00186 Cat. No.: HY-121381

K134 is a (PDE3) inhibitor. Kuraridine is a prenylated flavonol extract from

The IC50s of K134 toward PDE3A, PDE3B, PDE5, the roots of Sophora flavescens. Kuraridine has PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and an inhibitory effect on cGMP specific

>300 µM, respectively. phosphodiesterase type 5 (PDE5) (IC50=0.64 μM).

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

Kushenol B L791943 Cat. No.: HY-N8092 Cat. No.: HY-U00254

Kushenol B is an isoprenoid flavonoid isolated L791943 is a potent, selective Phosphodiesterase-4 from S. flavescens, has antimicrobial, (PDE4) inhibitor with an IC50 of 4.2 nM. anti-inflammatory and antioxidant activities. Kushenol B has inhibitory activity against cAMP phosphodiesterase (PDE), with an IC50 of 31 µM.

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

LAS-31180 LEO 39652 Cat. No.: HY-101811 Cat. No.: HY-131707

LAS-31180 is an inhibitor of phosphodiesterase 3, LEO 39652 is a dual-soft PDE4 inhibitor with with positive inotropic and vasodilator IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for properties. PDE4A, PDE4B, PDE4C and PDE4D, respectively.

LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) . Purity: >98% Purity: 99.11% 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, 50 mg, 100 mg

Levosimendan Lirimilast (Simsndan; OR-1259) Cat. No.: HY-14286 (BAY 19-8004) Cat. No.: HY-19672

Levosimendan (Simsndan; OR-1259) is a calcium Lirimilast (BAY 19-8004) is a potent, selective sensitiser used in the management of acutely and orally active phosphodiesterase-4 (PDE4) decompensated congestive failure. inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties. Purity: 99.51% Purity: ≥98.0% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

www.MedChemExpress.com 11

Lodenafil carbonate (Hydroxyhomosildenafil) Cat. No.: HY-123210 Cat. No.: HY-108045

Lodenafil is a potent phosphodiesterase type 5 Lodenafil carbonate, a dimer that acts as a (PDE5) inhibitor for the treatment of erectile delivering Lodenafil in vivo, is an orally dysfunction (ED). active phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).

Purity: 99.73% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Phase 4 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 1 mg, 5 mg

Lotamilast Mardepodect (RVT-501; E6005) Cat. No.: HY-12740 (PF-2545920) Cat. No.: HY-50098

Lotamilast (RVT-501; E6005) is a selective Mardepodect (PF-2545920) is a potent, orally

phosphodiesterase 4 (PDE4) inhibitor with an IC50 active and selective PDE10A inhibitor with an

of 2.8 nM. IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect can cross the blood-brain barrier.

Purity: ≥98.0% Purity: 99.86% 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, 50 mg, 100 mg

Mardepodect hydrochloride MBCQ (PF-2545920 hydrochloride) Cat. No.: HY-50098A Cat. No.: HY-114672

Mardepodect hydrochloride (PF-2545920 MBCQ is a potent and selective cGMP-specific hydrochloride) is a potent, orally active and phosphodiesterase (PDE V; PDE5) inhibitor with an

selective PDE10A inhibitor with an IC50 of 0.37 IC50 of 19 nM. MBCQ lacks inhibitory activity

nM, with >1000-fold selectivity over other toward other PDE (all IC50s>100 μM). PDEs. Mardepodect hydrochloride can cross the MBCQ dilates coronary arteries via specific blood-brain barrier. inhibition of cGMP-PDE. Purity: 95.10% Purity: 99.37% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 5 mg, 10 mg, 25 mg, 50 mg

Milrinone (Win 47203) Cat. No.: HY-14252 (SK3530) Cat. No.: HY-14930

Milrinone is a PDE3 inhibitor, and also an Mirodenafil(SK3530) is a phosphodiesterase type 5 and vasodilator. (PDE-5) inhibitor developed for the treatment of erectile dysfunction. Target: PDE5 Mirodenafil is a newly developed oral phosphodiesterase type 5 inhibitor.

Purity: 99.96% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 1 mg, 5 mg

Mirodenafil dihydrochloride MK-0952 (SK-3530 dihydrochloride) Cat. No.: HY-14930A Cat. No.: HY-11070

Mirodenafil dihydrochloride (SK3530 MK-0952 is a selective and orally active PDE4

dihydrochloride) is a phosphodiesterase type 5 inhibitor, with an IC50 of 0.53 nM. MK-0952 has (PDE-5) inhibitor developed for the treatment of the potential for Alzheimer’s disease study. erectile dysfunction. Target: PDE5 Mirodenafil is a newly developed oral phosphodiesterase type 5 inhibitor. Purity: 99.79% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

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

ML-030 Moracin M Cat. No.: HY-103050 Cat. No.: HY-122942

ML-030 is a potent PDE4 inhibitor, with IC50 of Moracin M, a phenolic component in the skin of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 Morus alba L., is a potent phosphodiesterase-4 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and (PDE4) inhibitor with IC50 values of 2.9, 4.5, PDE4D2, respectively. >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity. Purity: 98.04% Purity: 98.50% 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, 10 mg, 50 mg, 100 mg

MR-L2 MT-3014 Cat. No.: HY-128358 Cat. No.: HY-128349

MR-L2 is a reversible and noncompetitive MT-3014 is a potent, highly selective and allosteric activator of long-isoform brain-penetrated phosphodiesterase 10A (PDE 10A) phosphodiesterase-4 (PDE4), activates inhibitor, with IC50s of 0.062 nM and 0.09 nM for representative PDE4 long-isoform variants (PDE4A4, human PDE 10A and bovine PDE 10A, respectively. PDE4B1, PDE4C3, PDE4D5).

Purity: 99.36% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg

MY-5445 N-Methylbenzamide Cat. No.: HY-100933 Cat. No.: HY-135848

MY-5445 is a specific inhibitor of the cyclic GMP N-Methylbenzamide is a potent phosphodiesterase 10A phosphodiesterase, phosphodiesterase type 5 (PDE10A) inhibitor. N-Methylbenzamide has

(PDE5), with a Ki of 1.3 μM. MY-5445 inhibits anti-cancer activity. human aggregation.

Purity: 99.79% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 1 mg, 5 mg

Nortadalafil NPD-1335 (Demethyl Tadalafil) Cat. No.: HY-90009 Cat. No.: HY-126250

Nortadalafil is demethyl Tadalafil, which is a NPD1335 is a Trypanosoma brucei PDE5 inhibitor, currently marketed in pill form phosphodiesterase B1 (TbrPDEB1) inhibitor with for treating erectile dysfunction (ED) under the submicromolar activities against T. brucei name Cialis; and under the name Adcirca for the parasites. NPD1335 displays a greatly improved treatment of pulmonary arterial hypertension. IC50 cytotoxicity profile. value: Target:. Purity: 99.69% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg

NSP-805 Oglemilast Cat. No.: HY-19102 (GRC 3886) Cat. No.: HY-15178

NSP-805 is a potent and selective inhibitor of Oglemilast (GRC 3886) is a potent and orally guinea pig cardiac phosphodiesterase 3 (PDE3), and active phosphodiesterase-4 (PDE4) inhibitor a cardiotonic agent with vasodilator properties. with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Purity: ≥99.0% Purity: 98.20% Clinical Data: No Development Reported Clinical Data: Phase 2 Size: 10 mM × 1 mL, 5 mg, 10 mg, 20 mg Size: 5 mg, 10 mg, 50 mg

www.MedChemExpress.com 13

Olprinone Hydrochloride (Loprinone) Cat. No.: HY-14254A (Loprinone Hydrochloride) Cat. No.: HY-14254

Olprinone (Loprinone) is a potent phosphodiesterase Olprinone (Loprinone) Hydrochloride is a potent

(PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 phosphodiesterase (PDE) 3 inhibitor, with IC50s of and 14 μM for PDE1, PDE2, PDE3 and PDE4, 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and respectively. Olprinone is used for the research PDE4, respectively. of due to its positive inotropic and vasodilative effects. Anti-inflammatory activity. Purity: >98% Purity: 99.91% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Ophiobolin A OR-1855 Cat. No.: HY-N6781 Cat. No.: HY-W050000

Ophiobolin A, a fungal metabolite and a OR-1855, an active metabolite of Levosimendan, has phytotoxin, is a potent and irreversibly inhibitor effect on human myometrial contractility. of calmodulin-activated cyclic nucleotide Levosimendan is a calcium sensitiser used in the

phosphodiesterase, with an IC50 value of 9 μM. management of acutely decompensated congestive Ophiobolin A antimicrobial and anticancer heart failure. activity. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 100 mg

OR-1896 PAT-048 Cat. No.: HY-135746 Cat. No.: HY-123522

OR-1896 is an active long-lived metabolite of PAT-048 is a potent, selective and orally active Levosimendan. OR-1896 is a highly selective autotaxin inhibitor, inhibits IL-6 mRNA expression, phosphodiesterase (PDE) III isoform inhibitor and a but shows no effect on autotaxin protein and powerful vasodilator. OR-1896 can open pulmonary (LPA) production ATP-sensitive K+ channels and has Ca2+-sensitizing in lung fibrosis model. effect. Purity: 98.90% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg Size: 1 mg, 5 mg

PAT-505 PDE IV-IN-1 Cat. No.: HY-107781 Cat. No.: HY-U00352

PAT-505 is a potent, selective, noncompetitive and PDE IV-IN-1 is an inhibitor of phosphodiesterase IV,

orally available autotaxin inhibitor, with an IC50 used for the research of asthma, COPD or other of 2 nM in Hep3B cells, 9.7 nM in human blood and inflammatory diseases. 62 nM in mouse plasma.

Purity: 99.47% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

PDE-9 inhibitor PDE1-IN-2 Cat. No.: HY-50865 Cat. No.: HY-101490

PDE-9 inhibitor is useful for neurodegenerative PDE1-IN-2 is a PDE1 inhibitor extracted from diseases. patent WO2016/55618 A1, example 31. PDE1-IN-2 has

IC50 values of 6 nM, 140 nM and 164 nM for PDE1C, PDE1B and PDE1A, respectvely. PDE1-IN-2 is developed for the research of neurodegenerative disorders and psychiatric disorders. Purity: 99.83% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

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

PDE1-IN-3 PDE10-IN-1 Cat. No.: HY-130262 Cat. No.: HY-12813

PDE1-IN-3, compound 4 (WO2019156861), is a PDE10-IN-1 is a potent PDE10-IN-1 inhibitor selective human phosphodiesterase 1 (PDE1) extracted from Patent WO 2013192273 A1, for inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB treating CNS and metabolic disorders. with IC50 values of 23.99 μM and 10 μM, respectively.

Purity: >98% Purity: 97.82% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 50 mg

PDE10A-IN-2 hydrochloride PDE12-IN-1 Cat. No.: HY-131973 Cat. No.: HY-117318

PDE10A-IN-2 hydrochloride is a potent, highly PDE12-IN-1 is a potent and selective PDE12 selective and orally active phosphodiesterase 10A inhibitor with a pIC50 value for enzyme inhibition

(PDE10A) inhibitor with an IC50 of 2.8 nM. of 9.1. PDE12-IN-1 increases 2′,5′-linked

PDE10A-IN-2 hydrochloride shows selectivity of adenylate polymers (2-5A) levels, and the pEC50 >3500-fold against other PDE subtypes. value is 7.7. PDE12-IN-1 shows antiviral activity.

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

PDE12-IN-3 PDE2/PDE10-IN-1 Cat. No.: HY-124768 Cat. No.: HY-U00427

PDE12-IN-3 is a phosphodiesterase 12 (PDE12) PDE2/PDE10-IN-1 is a phosphodiesterase 2 (PDE2) inhibitor with a pXC50 of 7.68. Antiviral and PDE10 inhibitor with IC50s of 29 and 480 nM, activity. respectively.

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

PDE4B-IN-2 PDE5-IN-2 Cat. No.: HY-115687 Cat. No.: HY-112704

PDE4B-IN-2 is an orally active and selective PDE5-IN-2 is a potent, highly selective, and

PDE4B inhibitor (IC50=15 nM) and exhibits orally active PDE5 inhibitor, with an IC50 of >100-fold selectivity for PDE4B over 4D. 0.31 nM, less potently inhibits PDE2A, PDE10A,

PDE4B-IN-2 regulates cAMP in inflammatory cells PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 and inhibits LPS-induced TNF-α production and nM, respectively. Anti-pulmonary arterial accumulation in mouse . hypertension activity. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg

PDE9-IN-1 Cat. No.: HY-126137 (BL-191; PTX; Oxpentifylline) Cat. No.: HY-B0715

PDE9-IN-1 is a potent, selective, and orally Pentoxifylline (BL-191), a haemorheological agent, bioavailable phosphodiesterase-9A (PDE9A) is an orally active non-selective phosphodiesterase

Inhibitor with an IC50 of 8.7 nM. (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects.

Purity: >98% Purity: 99.90% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg, 1 g

www.MedChemExpress.com 15

PF-04447943 PF-04957325 Cat. No.: HY-15441 Cat. No.: HY-15426

PF-04447943 is a potent inhibitor of human PF-04957325 is a highly potent and selective PDE8

recombinant PDE9A (IC50=12 nM) with >78-fold inhibitor, with IC50s of 0.7 nM and 0.3 nM for selectivity, respectively, over other PDE family PDE8A and PDE8B, respectively.

members (IC50>1000 nM).

Purity: 99.97% Purity: 99.94% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

PF-05085727 PF-05180999 Cat. No.: HY-102050 Cat. No.: HY-111371

PF-05085727 is a potent, selective and brain PF-05180999 is a phosphodiesterase 2A (PDE2A)

penetrant inhibitor of cGMP-dependent PDE2A inhibitor, with an IC50 of 1.6 nM.

(IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.

Purity: 98.42% Purity: 99.94% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

PF-8380 Cat. No.: HY-13344 (RP 73401; RPR 73401) Cat. No.: HY-12887

PF-8380 is a potent autotaxin inhibitor with an Piclamilast (RP 73401) is a phosphodiesterase 4

IC50 of 2.8 nM in isolated enzyme assay and 101 nM (PDE4) inhibitor, with IC50 values of 16 nM and 2 in human whole blood. nM in pig aorta and soluble, respectively.

Purity: 98.95% 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

Pimobendan hydrochloride (UD-CG115) Cat. No.: HY-B0204 (UD-CG115 hydrochloride) Cat. No.: HY-B0204A

Pimobendan (UD-CG115) is a selective inhibitor of Pimobendan hydrochloride (UD-CG115 hydrochloride)

PDE3 with IC50 of 0.32 μM. is a selective inhibitor of PDE3 with IC50 of 0.32 μM.

Purity: 99.15% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg

Prinoxodan R 80123 (RGW2938) Cat. No.: HY-U00208 Cat. No.: HY-100615A

Prinoxodan (RGW2938) is a phosphodiesterase R 80123 is the Z-isomer of R 79595, is also a inhibitor. highly selective phosphodiesterase inhibitor. The fuction is similar to R 80122 (HY-100615, Revizinone).

Purity: 95.58% Purity: ≥98.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg Size: 1 mg

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

Revizinone Ro-15-2041 (R80122) Cat. No.: HY-100615 Cat. No.: HY-101807

Revizinone is a novel selective phosphodiesterase Ro 15-2041 is a selective platelet (PDE) inhibitor with IC50 values on this enzyme to phosphodiesterase inhibitor with antithrombotic 0.036 microM. properties.

Purity: 98.31% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Robustine Cat. No.: HY-N1343 Cat. No.: HY-15455

Robustine, a furoquinoline alkaloid, from Roflumilast is a selective PDE4 inhibitor with

Dictamnus albus, exhibits inhibitory potency IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, against human phosphodiesterase 5 (hPDE5A) in PDEA4, PDEB1, and PDEB2, respectively, without vitro. affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.

Purity: 99.95% Purity: 99.43% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

Roflumilast Impurity E Roflumilast N-oxide Cat. No.: HY-100640 Cat. No.: HY-100639

Roflumilast Impurity E is the impurity of Roflumilast N-oxide is a PDE type 4 inhibitor. Roflumilast. Roflumilast(Daliresp) is a drug which acts as a selective and long-acting inhibitor of the enzyme PDE-4 with an IC50 value of 0.8 nM.

Purity: >98% Purity: 99.54% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg, 10 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Rolipram Saterinone hydrochloride ((R,S)-Rolipram; SB 95952; ZK 62711) Cat. No.: HY-16900 (BDF 8634 hydrochloride) Cat. No.: HY-101644A

Rolipram is a selective phosphodiesterases PDE4 Saterinone hydrochloride is a phosphodiesterase III inhibitor with IC50s of 3 nM, 130 nM and 240 nM (PDE III) inhibitor. for PDE4A, PDE4B, and PDE4D, respectively.

Purity: 99.90% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Sch59498 SDZ-MKS 492 Cat. No.: HY-U00374 (MKS 492) Cat. No.: HY-100164

Sch59498 is a potent inhibitor of phosphodiesterase SDZ-MKS 492 (MKS 492) is a selective inhibitor of 1c (Pde1c). cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and . Purity: >98% Purity: 98.07% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

www.MedChemExpress.com 17

Senazodan Cat. No.: HY-101693 (SKF 94836) Cat. No.: HY-19026

Senazodan is a Ca2+ sensitiser, and also shows Siguazodan (SKF 94836) is a potent, selective and inhibition effect on PDE III. orally active phosphodiesterase III (PDE-III)

inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact

with an EC50 of 18.88 μM.

Purity: >98% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 5 mg, 10 mg

Sildenafil Sildenafil citrate (UK-92480) Cat. No.: HY-15025 (UK-92480 citrate) Cat. No.: HY-15025A

Sildenafil (UK-92480) is a potent Sildenafil citrate is a potent phosphodiesterase

phosphodiesterase type 5 (PDE5) inhibitor with an type 5 (PDE5) inhibitor with IC50 of 5.22 nM.

IC50 of 5.22 nM.

Purity: 99.89% Purity: 99.97% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg

Sophoflavescenol Sp-cAMPS Cat. No.: HY-N2284 Cat. No.: HY-100530B

Sophoflavescenol is a prenylated flavonol, which Sp-cAMPS, a cAMP analog, is potent activator of

shows great inhibitory activity with IC50 of 0.013 cAMP-dependent PKA I and PKA II. Sp-cAMPS is also μM against Phosphodiesterase 5 (PDE5), and also a potent, competitive phosphodiesterase (PDE3A)

inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the

with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 PDE10 GAF domain with an EC50 of 40 μM. µM, 8.37 µM and 8.21 µM, respectively. Purity: 98.15% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Sp-cAMPS sodium salt Tadalafil Cat. No.: HY-100530C (IC-351) Cat. No.: HY-90009A

Sp-cAMPS sodium salt, a cAMP analog, is potent Tadalafil (IC-351) is a PDE5 inhibitor with an

activator of cAMP-dependent PKA I and PKA II. IC50 value of 1.8 nM. Sp-cAMPS sodium salt is also a potent, competitive

phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF

domain with an EC50 of 40 μM. Purity: 98.72% Purity: 99.96% Clinical Data: No Development Reported Clinical Data: Launched Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 50 mg, 100 mg

TAK-915 TDP1 Inhibitor-1 Cat. No.: HY-103493 Cat. No.: HY-119372

TAK-915 is a potent, selective, brain-penetrant TDP1 Inhibitor-1 is a potent Tyrosyl-DNA

and orally active phosphodiesterase 2A (PDE2A) Phosphodiesterase 1 (TDP1) inhibitor with an IC50

inhibitor with an IC50 of 0.61 nM. TAK-915 is of 7 μM. >4100-fold more selectivity for PDE2A than PDE1A.

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

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

Theodrenaline Theophylline ((±)​-​) Cat. No.: HY-U00344 (1,3-Dimethylxanthine; Theo-24) Cat. No.: HY-B0809

Theodrenaline is a cardiac , also acts as Theophylline is a nonselective phosphodiesterase an anti-hypotensive agent together with . (PDE) inhibitor, adenosine receptor blocker, and histone deacetylase (HDAC) activator.

Purity: >98% Purity: 99.94% Clinical Data: Launched Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 500 mg, 5 g

Thioquinapiperifil Thioquinapiperifil dihydrochloride (KF31327 free base) Cat. No.: HY-119611 (KF31327) Cat. No.: HY-119611A

Thioquinapiperifil (KF31327 free base), a potent, Thioquinapiperifil dihydrochloride (KF31327), a selective and non-competitive phosphodiesterase-5 potent, selective and non-competitive

(PDE-5, IC50 of 0.074 nM) inhibitor, is used for phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) sexual enhancement study. inhibitor, is used for sexual enhancement study.

Purity: >98% Purity: 99.18% 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, 50 mg, 100 mg

THPP-1 Tibenelast sodium Cat. No.: HY-117604 (LY 186655) Cat. No.: HY-101705

THPP-1, a SGC chemical probe, is a potent and Tibenelast sodium is a phosphodiesterase inhibitor. orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species. Purity: 98.95% 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

TP-10 TPN171 Cat. No.: HY-14550 Cat. No.: HY-128593

TP-10 is a PDE10A inhibitor with IC50 of 0.8 nM. TPN171 is a potent, selective and oral bioavailable inhibitor of phosphodiesterase type 5

(PDE5) with an IC50 of 0.62 nM, being developed for the treatment of pulmonary arterial hypertension (PAH).

Purity: 98.54% Purity: >98% Clinical Data: Phase 2 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Trequinsin hydrochloride TyK2-IN-2 (HL 725) Cat. No.: HY-18740A Cat. No.: HY-101762

Trequinsin hydrochloride (HL 725) is an extremely TyK2-IN-2 (Compoud 18) is a potent and selective potent inhibitor of platelet CAMP phosphodiesterase TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and

(PDE), with an IC50 of 0.25 nM. 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits

phosphodiesterase 4 (PDE4) with an IC50 of 62 nM.

Purity: 99.96% Purity: 99.71% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg

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Udenafil (DA8159) Cat. No.: HY-18253 Cat. No.: HY-B0442

Udenafil (DA8159) is a potent, selective and Vardenafil is a selective, orally active, potent orally active phosphodiesterase type 5 (PDE5) inhibitor of phosphodiesterase-5 (PDE5), with an

inhibitor. Udenafil also inhibits cGMP IC50 of 0.7 nM. Vardenafil shows selectivity over and can be used for erectile dysfunction research. PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM).

Purity: 99.73% Purity: >98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 1 mg, 5 mg

Vardenafil hydrochloride Cat. No.: HY-B0442A (OPC-8212) Cat. No.: HY-15297

Vardenafil hydrochloride is a selective, orally Vesnarinone is a quinolinone derivative, and its active, potent inhibitor of phosphodiesterase-5 pharmacodynamic effects include inhibition of

(PDE5), with an IC50 of 0.7 nM. Vardenafil phosphodiesterase III (PDE3) activity, increases hydrochloride shows selectivity over PDE1 (180 in calcium flux and decreases in flux. nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Purity: 99.51% Purity: 96.06% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 200 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Vinpocetine VP3.15 (Ethyl apovincaminate) Cat. No.: HY-13295 Cat. No.: HY-128879

Vinpocetine (Ethyl apovincaminate) is a derivative VP3.15 is a potent, orally bioavailable and of the alkaloid Vincamine that blocks CNS-penetrant dual phosphodiesterase (PDE)7- + voltage-gated Na channels. The IC50 value of glycogen synthase kinase (GSK)3 inhibitor, with

Vinpocetine on direct IKK inhibition in the IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, cell-free system is 17.17 μM. respectively.

Purity: 99.77% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg, 200 mg, 500 mg Size: 1 mg, 5 mg

VP3.15 dihydrobromide W-7 hydrochloride Cat. No.: HY-128879A Cat. No.: HY-100912

VP3.15 dihydrobromide is a potent, orally W-7 hydrochloride is a selective calmodulin bioavailable and CNS-penetrant dual antagonist. W-7 hydrochloride inhibits the phosphodiesterase (PDE)7- glycogen synthase kinase Ca2+-calmodulin-dependent phosphodiesterase and

(GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 myosin light chain kinase with IC50 values of 28 μM for PDE7 and GSK-3, respectively. μM and 51 µM, respectively. W-7 hydrochloride induces apoptosis and has antitumor activity. Purity: 98.22% Purity: 99.65% 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, 25 mg, 50 mg

WAY127093B racemate Win 58237 Cat. No.: HY-101749 Cat. No.: HY-101661

WAY127093B racemate is the racemate of WAY127093B. Win 58237 is a cyclic nucleotide phosphodiesterase

WAY127093B is an orally active phosphodiesterase IV (PDE) inhibitor, with Ki of 170 nM for PDE V, inhibitor in guinea pigs and rats. possessing vasorelaxant activity.

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

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

Win-62005 Cat. No.: HY-U00136 (M&B 22948) Cat. No.: HY-B1816

Win-62005 is a cyclic AMP phosphodiesterase III Zaprinast (M&B 22948) is an inhibitor of

(PDE III) inhibitor with Kis of 25 and 26 nM for cGMP-selective Phosphodiesterases(PDEs). Zaprinast rat heart and canine aorta, respectively. is a G protein-coupled receptor (GPR) 35 agonist which activates rat GPR35 strongly and activates human GPR35 moderately.

Purity: >98% Purity: 99.80% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg

Zardaverine Ziritaxestat Cat. No.: HY-15485 (GLPG1690) Cat. No.: HY-101772

Zardaverine is a newly developed dual-selective Ziritaxestat (GLPG1690) is a first-in-class

PDE3/4 inhibitor with IC50 values of 0.5 uM and autotaxin (ATX) inhibitor, with an IC50 of 131 nM

0.8 uM respectively. and a Ki of 15 nM.

Purity: 98.64% Purity: 99.97% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

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