Bioactivity | 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]. |
Invitro | 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]. |
Name | PDE5-IN-2 |
CAS | 2244517-61-9 |
Formula | C25H21N3O6S |
Molar Mass | 491.52 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |