2244517-61-9

2244517-61-9 structure

Name: PDE5-IN-2
Chemical Name: PDE5-IN-2
CAS Number: 2244517-61-9
Molecular Formula: C₂₅H₂₁N₃O₆S
Molecular Weight: 491.52
Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
Create Date: 2019-06-01 13:45:45
Modify Date: 2024-01-10 12:19:38
PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].

Name	PDE5-IN-2

Description	PDE5-IN-2 is a potent, highly selective, and orally active PDE5 inhibitor, with an IC50 of 0.31 nM, less potently inhibits PDE2A, PDE10A, PDE4D2, and PDE6C, with IC50s of 106, 46, 43, 1.2 nM, respectively. Anti-pulmonary arterial hypertension activity[1].
Related Catalog	Research Areas >> Cardiovascular Disease Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)
Target	PDE5A1:0.31 nM (IC50) PDE6C:1.2 nM (IC50) PDE4D2:43 nM (IC50) PDE10A:46 nM (IC50) PDE2A:106 nM (IC50)
In Vitro	PDE5-IN-2 (Compound 3) has at least 1000-fold selectivity over PDE1B, PDE3A, PDE7A1, PDE8A1, and PDE9A2 (IC50s, >32 000 nM)[1].
In Vivo	PDE5-IN-2 (1.25 mg/kg, p.o.) shows anti-pulmonary arterial hypertension activity, decreases mean pulmonary artery pressure in rats[1].
References	[1]. Wu D, et al. Optimization of Chromeno[2,3- c]pyrrol-9(2 H)-ones as Highly Potent, Selective, and Orally Bioavailable PDE5 Inhibitors: Structure-Activity Relationship, X-ray Crystal Structure, and Pharmacodynamic Effect on Pulmonary Arterial Hypertension. J Med Chem. 2018 Sep 27;61(18):8468-8473.

Molecular Formula	C₂₅H₂₁N₃O₆S
Molecular Weight	491.52