Name | Norverapamil hydrochloride |
Description | Norverapamil hydrochloride (D591 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. |
In vitro | Norverapamil inhibits macrophage-induced tolerance and attains serum levels comparable to verapamil. Both verapamil and its primary metabolite, Norverapamil, are identified as mechanism-based inhibitors and substrates of CYP3A, exhibiting non-linear pharmacokinetics clinically. Furthermore, ((±)-Norverapamil hydrochloride) proves as effective as verapamil in inhibiting tolerance and killing intracellular M. tuberculosis in monotherapy, matching its efficacy against isoniazid and rifampicin tolerance [1][3]. |
In vivo | Norverapamil hydrochloride (9 mg/kg; p.o.) exhibits a terminal half-life of 9.4 hours, an AUC of 260 ng ml−1 h, and a Cmax of 41.6 ng/mL[4]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | H2O : 50 mg/mL (104.81 mM) DMSO : 31 mg/mL (64.98 mM)
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Keywords | 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 |
Inhibitors Related | L-Ascorbic acid | Isonicotinic acid | 1-Octanol |
Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Neuroprotective Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library |