盐酸去甲维拉帕米 T16339

Product Introduction
Bioactivity


英文名: Norverapamil hydrochloride

描述: Norverapamil hydrochloride (D591 hydrochloride) 是 Verapamil 的 N-去甲基代谢物，是 L 型钙通道阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。

体外活性: Norverapamil also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil. 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 the clinic. Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs [1][3].

体内活性: Norverapamil hydrochloride（9 mg/kg；p.o.）的终末半衰期、AUC及Cmax值分别为9.4小时、260 ngh/ml与41.6 ng/mL[4]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 50 mg/mL (104.81 mM)
DMSO : 31 mg/mL (64.98 mM)


关键字: MDR1 | CD243 | Inhibitor | mycobacterial | Norverapamil | M. tuberculosis | Multidrug resistance protein 1 | D 591 Hydrochloride | Ca2+ channels | metabolite | (±)-Norverapamil | P-gp | D-591 Hydrochloride | Calcium Channel | efflux | D591 Hydrochloride | Ca channels | Drug Metabolite | P-glycoprotein | inhibit | Norverapamil Hydrochloride | ABCB1 | Cluster of differentiation 243 | D 591 | Norverapamil hydrochloride | pumps | D-591 | D591 | Pgp

相关产品: Myoregulin | AE0047 Hydrochloride | CP-060 | PD 0299685 | O-1602 | ZSET1446 | Acetylcholine chloride | LY393615 | Devapamil | PD173212

相关库: Ion Channel Inhibitor Library | Anti-Hypertension Compound Library | Anti-Cancer Compound Library | Calcium Channel Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | Inhibitor Library | NO PAINS Compound Library | Drug Metabolite/Impurity Library

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