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| 中文名称 |
Vardenafil hydrochloride
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|---|---|
| 中文别名 |
瓦地拉非盐酸盐;盐酸伐地那非;2-[2-乙氧基-5-(4-乙基哌嗪-1-基)磺酰苯基]-5-甲基-7-丙基-1H-咪唑并[5,1-f][1,2,4]三嗪-4-酮盐酸盐;vardenafil盐酸盐;奥氮平杂质;伐地那非;伐地那非(甾体);伐地那非盐酸盐;科研实验盐酸伐地那非;临床实盐酸伐地那非;瓦地拉非盐酸盐 盐酸伐地那非;瓦地拉非盐酸盐(甾体);瓦地那非;盐酸伐地那非粉末;盐酸伐地那非固体状;盐酸伐地那非中间体;医药级盐酸伐地那非;伐他那非盐酸盐
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| 英文名称 |
Vardenafil hydrochloride
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| 英文别名 |
Vardenafil hydrochloride;2-[2-Ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-5-methyl-7-propyl-1H-imidazo[5,1-f][1,2,4]triazin-4-one hydrochloride;Vardenafil, Hydrochloride Salt Discontinued See V098001;Vardenafil;Vardenafil (hydrochloride);Vardenafil, Hydrochl;Levitra,Valdenafil;Levitra,Valdenafil.HCl;Nuviva;VARDENAFIL HCL;VARDENAFIL,HYDROCHLORIDE SALT;VARDENAFILMONOHYDROCHLORIDE(SUBJECTTOPATENTFREE)
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| Cas No. |
224785-91-5
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| 分子式 |
C23H32N6O4S.HCl
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| 分子量 |
525.06
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| 包装储存 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 产品详情 |
Vardenafil hydrochloride 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 对 PDE1 (180 nM)，PDE6 (11 nM) ，PDE2，PDE3，PDE4 (>1000 nM) 有不同的抑制作用。Vardenafil hydrochloride 非竞争性地抑制环磷酸鸟苷 (cGMP) 水解，从而提高 cGMP 水平。Vardenafil hydrochloride 可用于研究勃起功能障碍、肝炎、糖尿病等疾病。
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|---|---|
| 生物活性 |
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC 50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research like erectile dysfunction, hepatitis, diabetes.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
PDE5 0.7 nM (IC50) PDE6 11 nM (IC50
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| 体外研究(In Vitro) |
Vardenafil hydrochloride specifically inhibits the hydrolysis of cGMP by PDE5 with an IC50 of 0.7 nM.Vardenafil hydrochloride increases intracellular cGMP levels in the cavernosum tissue of the penis, thus results increasing the dilation of the bodys sinuses and blood flow. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
Vardenafil hydrochloride (I.V.; 0.03 mg/kg) exhibits facilitator effects in rats with cavernous nerve injury.
Vardenafil hydrochloride (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 (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. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| ClinicalTrial |
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| 参考文献 |
[1]. Saenz de Tejada I, et al. The phosphodiesterase inhibitory selectivity and the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Int J Impot Res. 2001;13(5):282-290.[2]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.
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| 溶解度数据 |
In Vitro: DMSO : 100 mg/mL (190.45 mM; Need ultrasonic)H2O : ≥ 100 mg/mL (190.45 mM)
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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