Avanafil  330784-47-9

Avanafil
分子式：C23H26ClN7O3   分子量：483.95
 
產品描述
Avanafil是一種高度選擇性PDE5抑制劑，IC50為1nM.
靶點
PDE5
         
IC50
1 nM
         
體外研究
Avanafil (T-1032) is a specific inhibitor of PDE5 with IC50 of 1 nM in a competitive manner. Avanafil binds to the catalytic site of PDE5 and inhibits cGMP hydrolysis. Avanafil also inhibits PDE6 with IC50 of 28 nM. In contrast, the IC50 values of avanafil for PDE1, PDE2, PDE3 and PDE4 are more than 1μM. Avanafil increases the intracellular concentrations of cGMP with and without CNP in cultured rat VSMCs.
體內研究
Intravenous (1-100 μg/kg) and intraduodenal (3, 30, 300 μg/kg) treatment with Avanafil dose dependently potentiates the tumescence induced by pelvic nerve stimulation in dogs. Furthermore, i.v. Avanafil augments the tumescence induced by sodium nitroprusside (SNP) but not by vasoactive intestinal polypeptide (VIP).
溶解性
DMSO 97 mg/mL，水 <1 mg/mL，乙醇 <1 mg/mL
穩定性
2年 -20°C粉狀，6月-80°C溶于DMSO
特征
Avanafil is highly selective for PDE5.