Vardenafil 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 对 PDE1、PDE6 的IC50为 180 nM，11 nM，对 PDE3、PDE4 的IC50>1000 nM。Vardenafil 非竞争性地抑制环磷酸鸟苷 (cGMP) 水解，从而提高 cGMP 水平。Vardenafil 可用于研究勃起功能障碍、肝炎、糖尿病等疾病。
| 生物活性 | Vardenafil is a selective and orally active inhibitor ofphosphodiesterase-5(PDE5), with anIC50of 0.7 nM. Vardenafil shows inhibitory towardsPDE1,PDE6withIC50s of 180 nM, and 11 nM, whileIC50s are >1000 nM forPDE3andPDE4[1]. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels[2]. Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes[1]-[6]. |
| IC50& Target[2] | PDE5 0.7 nM (IC50) | PDE6 11 nM (IC50) | PDE1 180 nM (IC50) |
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体外研究
(In Vitro) | Vardenafil specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50of 0.7 nM[1].
Vardenafil 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 (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury[4].
Vardenafil (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 (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 | 4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(51.17 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.0467 mL | 10.2333 mL | 20.4666 mL | | 5 mM | 0.4093 mL | 2.0467 mL | 4.0933 mL | | 10 mM | 0.2047 mL | 1.0233 mL | 2.0467 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.12 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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