Vardenafil-d5(Synonyms: 伐地那非-d5杂质17)

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Vardenafil-d5 (Synonyms: 伐地那非-d5杂质17)

Vardenafil-d5 是 Vardenafil 氘代物。Vardenafil 是一种高选择性、具有口服活性的、有效的磷酸二酯酶5 (PDE5) 抑制剂,IC50 为 0.7 nM。Vardenafil 对 PDE1 (180 nM),PDE6 (11 nM),PDE2,PDE3,PDE4 (>1000 nM) 具有选择性。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。

Vardenafil-d5(Synonyms: 伐地那非-d5杂质17)

Vardenafil-d5 Chemical Structure

CAS No. : 1189685-70-8

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生物活性

Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

493.63

Formula

C23H27D5N6O4S

CAS 号

1189685-70-8

中文名称

伐地那非-d5杂质17

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.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Ashour AE, et al. Vardenafil dihydrochloride. Profiles Drug Subst Excip Relat Methodol. 2014;39:515-544.

    [3]. 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.

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