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Vardenafil hydrochloride trihydrate
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Vardenafil hydrochloride trihydrate图片
CAS NO: 330808-88-3
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 介绍
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。
生物活性

Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor ofphosphodiesterase-5(PDE5), with anIC50of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towardsPDE1,PDE6withIC50s of 180 nM, and 11 nM, whileIC50s are >1000 nM forPDE3andPDE4[1]. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels[2]. Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6].
IC50& Target

PDE5

0.7 nM (IC50)

PDE1

180 nM (IC50)

PDE6

11 nM (IC50)
体外研究
(In Vitro)

Vardenafil hydrochloride trihydrate specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50of 0.7 nM[1].
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[3].
体内研究
(In Vivo)

Vardenafil hydrochloride trihydrate (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury[4].
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-κB and iNOS in hepatic tissue[5].
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[6].

Animal Model: Male rat (9-week-old) underwent surgery for laparotomy or bilateral cavernous nerve (CN) crush injury[4]
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)[5]
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)[6]
Dosage: 10 mg/kg
Administration: Oral gavage; once daily, for 25 weeks
Result: Improved myofilament function in diabetic rat hearts.
分子量

579.11
Formula

C23H39ClN6O7S
CAS 号

330808-88-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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