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CAS No. : 330808-88-3
MCE 国际站:Vardenafil hydrochloride trihydrate
产品活性:Vardenafil hydrochloride trihydrate 是一种具有高选择性和口服活性的磷酸二酯酶 5 (PDE5) 抑制剂,IC50 为 0.7 nM。Vardenafil hydrochloride trihydrate 对 PDE1、PDE6 的 IC50 为 180 nM,11 nM,对 PDE3、PDE4 的 IC50 >1000 nM。Vardenafil hydrochloride trihydrate 非竞争性地抑制环磷酸鸟∑苷 (cGMP) 水解,从而提高 cGMP 水平。Vardenafil hydrochloride trihydrate 可用于研究勃起功能障碍、肝炎、糖尿病等疾病。
研究领域:Metabolic Enzyme/Protease
作用靶点:Endogenous Metabolite | Phosphodiesterase (PDE)
In Vitro: Vardenafil hydrochloride trihydrate specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM.
Vardenafil hydrochloride trihydrate increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the body's sinuses and blood flow.
In Vivo: Vardenafil hydrochloride trihydrate (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury.
Vardenafil hydrochloride trihydrate (I.V.; 0.17 mg/kg once daily; 7 days) protects liver against Con A–induced hepatitis, and decreases the expression of NF-B and iNOS in hepatic tissue.
Vardenafil hydrochloride trihydrate (P.O.; 10 mg/kg once daily; 25 weeks) prevents the reduction of tissue cGMP levels and the increase in 3-NT generation in ZDF hearts.
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