Vardenafil hydrochloride trihydrate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

伐地那非盐酸盐三水合物是一种新型 PDE 抑制剂，对 PDE5 和 PDE1 的 IC50 分别为 0.7 和 180 nM。

Vardenafil, also known as BAY 38-9456, is a PDE5 inhibitor used for treating erectile dysfunction. Vardenafil (VAR) is synthetic, highly selective, and potent inhibitor of phosphodiesterase-5 which competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. It is clinically approved for treatment of erectile dysfunction in men, including diabetic and postprostatectomy patients.(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.

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.

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. Animal Model:Male rat (9-week-old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury Dosage:0.03 mg/kg Administration:Intravenous injection Result:Restored normal erectile responses with a combind administration of BAY 60-4552 (0.03, 0.3 mg/kg).Animal Model:Liver injury induced by Con A in male Swiss albino mice (20 ± 2 g)Dosage:0.17 mg/kg Administration:Intravenous injection; once daily, for 7 days; as a pretreatment Result:Reduced the levels of serum transaminases and alleviated Con A-induced hepatitis.Animal Model:Male 7-week-old Zucker diabetic fatty (ZDF) rats (preserved ejection fraction, HFpEF)Dosage:10 mg/kg Administration:Oral gavage; once daily, for 25 weeks Result:Improved myofilament function in diabetic rat hearts.

BAY 38-9456 | Vardenafil HCl | Levitra | Staxyn | Vivanza

Others

Other Targets

PDE1| PDE5

Cardiovascular Disease

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330808-88-3

579.11

C23H32N6O4S·HCl·3H2O

>98% (HPLC)

——

n12[nH]c(nc(=O)c1c(nc2CCC)C)c1c(ccc(c1)S(=O)(=O)N1CCN(CC1)CC)OCC.Cl.O.O.O

2-(2-ethoxy-5-((4-ethylpiperazin-1-yl)sulfonyl)phenyl)-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(1H)-one dihydrochloride trihydrate

(-20℃)

With Ice Pack

≥ 2 years