| Bioactivity | PDE5-IN-13 inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for the treatment of PAH (pulmonary arterial hypertension). PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 has reasonable drug-like profiles[1]. |
| Invitro | PDE5-IN-13 的 C3 氰化物基团通过水分子与 D76 4和 H613 形成氢键桥，这稳定了 PDE5-IN-13 结合构象[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PDE5-IN-13 相关抗体: |
| In Vivo | PDE5-IN-13 (1500 mg/kg, p.o.) 在鼠中无急性毒性[1]。PDE5-IN-13 (5.0 mg/kg, p.o. , 每天, 21天) 在 Monocrotalin (HY-N0750) 诱导的肺动脉高压大鼠模型中，对增加 mPAP (肺动脉高压) 和 减少 RVHI (右心室肥大指数) 的药效比 Sildenafil citrate (HY-15025A) (10.0mg/kg) 好得多[1]。PDE5-IN-13 的体内药代动力学特性。PK parameters |
| Formula | C31H26N4O2 |
| Molar Mass | 486.56 |
| 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]. Zhang B, et.al. Discovery and Optimization of Dihydroquinolin-2(1H)-ones as Novel Highly Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension. J Med Chem. 2024 Dec 26;67(24):22134-22144. |