| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.19 mM), Sonication is recommended.
H2O : 50 mg/mL (104.81 mM), Sonication is recommended.
DMSO : 31 mg/mL (64.98 mM), Sonication is recommended.
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| Keywords | pumps | P-gp (P-glycoprotein) | P-gp | Pgp | P-glycoprotein (P-gp) inhibitor | P-glycoprotein | Norverapamil Hydrochloride | Norverapamil | mycobacterial | Multidrug resistance protein 1 | metabolite | MDR1 | M. tuberculosis | Inhibitor | inhibit | efflux | DrugMetabolite | Drug Metabolite | D-591 Hydrochloride | D591 Hydrochloride | D-591 | D591 | D 591 Hydrochloride | D 591 | Cluster of differentiation 243 | CD243 | CalciumChannel | Calcium channel blocker | Calcium channel | Ca2+ channels | Ca channels | ABCB1 | (±)-Norverapamil |
| Inhibitors Related | Quadrol | 2-(Methylamino)benzoic acid | 2,4,6-Tri-tert-butylphenol | Chlorocresol | L-Ascorbic acid | 10-Undecen-1-ol | Isonicotinic acid | L-Ascorbic acid sodium salt | 2-Nitrobenzoic acid | Magnesium Chloride Hexahydrate | Lansoprazole sulfide | Magnesium sulfate |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Neuroprotective Compound Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | Bioactive Compounds Library Max | Drug Metabolite/Impurity Library | Ion Channel Targeted Library | Anti-Cancer Compound Library | Anti-Hypertension Compound Library |
United States
