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Datasheet Inhibitors / Agonists / Screening Libraries a DRUG SCREENING EXPERT Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT Product Name : Norverapamil hydrochloride Catalog Number : T16339 CAS Number : 67812-42-4 Molecular Formula : C26H37ClN2O4 Molecular Weight : 477.04 Description: Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor. Storage: 2 years -80°C in solvent; 3 years -20°C powder; H2O 50 mg/mL (104.81 mM) Solubility DMSO 31 mg/mL (64.98 mM) ( < 1 mg/ml refers to the product slightly soluble or insoluble ) Calcium channel blocker;P- glycoprotein (P-gp) inhibitor Receptor (IC50) Calcium channel blocker P-gp (P-glycoprotein) In vitro Activity 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]. In vivo Activity Norverapamil hydrochloride (9 mg/kg; p.o.) has a terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng▪h/ml, and 41.6 ng/mL, respectively[4]. Reference 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. Pauli-Magnus C, et al. Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000 May;293(2):376-82. 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. 4. Choi DH, et al. Effects of simvastatin on the pharmacokinetics of verapamil and its main metabolite, norverapamil, in rats. Eur J Drug Metab Pharmacokinet. 2009 Jul-Sep;34(3-4):163-8. FOR RESEARCH PURPOSES ONLY. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE. Information for product storage and handling is indicated on the product datasheet. Targetmol products are stable for long term under the recommended storage conditions. Our products may be shipped under different conditions as many of them are stable in the short-term at higher or even room temperatures. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, please follow the storage recommendations on the product data sheet. [email protected] | Tel: +1-781-999-4286 | www.targetmol.com Datasheet Inhibitors / Agonists / Screening Libraries A DRUG SCREENING EXPERT [email protected] | Tel: +1-781-999-4286 | www.targetmol.com.
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