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) |
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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].
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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. |
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| 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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