二盐酸伐地那非 T4480

Product Introduction
Bioactivity


英文名: Vardenafil dihydrochloride

描述: Vardenafil dihydrochloride (Levitra) 是一种新型 PDE 抑制剂，对 PDE5 和 PDE1 的 IC50 分别为 0.7 和 180 nM。

体外活性: Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM (6.6 nM). Vardenafil significantly enhances the SNP-induced relaxation of human trabecular smooth muscle at 3 nM (10 nM). Vardenafil also significantly potentiates both ACh-induced and transmural electrical stimulation-induced relaxation of trabecular smooth muscle. Vardenafil (100 mM) increases cyclic GMP levels in rat hippocampal slices. Vardenafil, tadalafil, and Sildenafil each competitively inhibit cGMP hydrolysis by phosphodiesterase-5 (PDE5), thereby fostering cGMP accumulation and relaxation of vascular smooth muscle.

体内活性: Vardenafil dose-dependently potentiates erectile responses to intravenously administered sodium nitroprusside in rabbit. Vardenafil (3 mg/kg, p.o.) results in an improved object discrimination performance in rats. Vardenafil (30 mg/L, p.o.) increases both iNOS and proliferating cell nuclear antigen expression (SM cell replication) in rats, with normalization of the dynamic infusion cavernosometry drop rate and SM/collagen ratio. Vardenafil induces powerful preconditioning-like cardioprotective effect against ischemia/reperfusion injury through the opening of mitochondrial K(ATP) channels in the heart of rabbit. Vardenafil protects the ischemic myocardium against reperfusion injury through a mechanism dependent on mitochondrial K(ATP) channel opening.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 10 mg/mL (17.27 mM)
Ethanol : 16 mg/mL (27.6 mM)
DMSO : 93 mg/mL (160.6 mM)


关键字: cGMP | erectile dysfunction | impotence | Vardenafil | Pharmacokinetics | erectile | selective | zucker diabetic fatty rats | inhibit | smooth | diabetes | Inhibitor | Endogenous Metabolite | Vardenafil dihydrochloride | hepatitis | dysfunction | muscle | stimulation | Vardenafil Dihydrochloride | Phosphodiesterase (PDE)

相关产品: Crisaborole | Ginkgolide J | TAK-915 | uk-50001 | Vardenafil | Lotamilast | Enpp-1-IN-16 | BRL-50481 | D159687 | Oglemilast

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途