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Norverapamil hydrochloride((±)-Norverapamil hydrochloride)
本产品不向个人销售,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。
Norverapamil hydrochloride((±)-Norverapamil hydrochloride)图片
CAS NO:67812-42-4
规格:98%
分子量:477.04
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议

产品介绍
Norverapamil是一个钙通道阻滞剂,是verapamil主要的活性代谢物。
CAS:67812-42-4
分子式:C26H37ClN2O4
分子量:477.04
纯度:98%
存储:Store at -20°C

Background:

Norverapamil is a calcium channel blocker, it is the main active metabolite of verapamil.In vitro: Norverapamil is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil.[1] Norverapamil (NOR) is the major metabolite and shows approximately 20% of the efficacy of VER with regard to the vasodilation effect, but shows no antiarrhythmic activity. [2] Verapamil and its major metabolite norverapamil were identified to be both mechanism-based inhibitors and substrates of CYP3A and reported to have non-linear pharmacokinetics in clinic. [3]




[1]. Adams KN et al. Verapamil, and its metabolite norverapamil, inhibit macrophage-induced, bacterial efflux pump-mediated tolerance to multiple anti-tubercular drugs. J Infect Dis. 2014 Aug 1;210(3):456-66. [2]. Singhal P et al. Enantiomeric separation of verapamil and its active metabolite, norverapamil, and simultaneous quantification in human plasma by LC-ESI-MS-MS. J Chromatogr Sci. 2012 Oct;50(9):839-48. [3]. Wang J et al. A semi-physiologically-based pharmacokinetic model characterizing mechanism-based auto-inhibition to predict stereoselective pharmacokinetics of verapamil and its metabolite norverapamil in human. Eur J Pharm Sci. 2013 Nov 20;50(3-4):290-302.