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Norverapamil hydrochloride

Catalog No. T16339 CAS 67812-42-4

Synonyms: (±)-Norverapamil hydrochloride, D591 hydrochloride

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.

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Norverapamil hydrochloride Chemical Structure

Norverapamil hydrochloride, CAS 67812-42-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 53.00
2 mg	In stock	$ 77.00
5 mg	In stock	$ 117.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 451.00
50 mg	In stock	$ 663.00
100 mg	In stock	$ 937.00
1 mL * 10 mM (in DMSO)	In stock	$ 123.00

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Purity: 99.63%

Biological Description

Chemical Properties

Storage & Solubility Information

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.) has a terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng?h/ml, and 41.6 ng/mL, respectively[4].

Synonyms	(±)-Norverapamil hydrochloride, D591 hydrochloride
Molecular Weight	477.04
Formula	C26H37ClN2O4
CAS No.	67812-42-4

Storage

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

Solubility Information

H2O: 50 mg/mL (104.81 mM)

DMSO: 31 mg/mL (64.98 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Neuronal Signaling Compound Library Bioactive Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Ion Channel Inhibitor Library Calcium Channel Compound Library Metabolism Compound Library Anti-Cardiovascular Disease Compound Library Anti-Hypertension Compound Library

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Keywords

Norverapamil hydrochloride 67812-42-4 Membrane transporter/Ion channel Metabolism Neuroscience Drug Metabolite P-gp Calcium Channel MDR1 CD243 Inhibitor mycobacterial Norverapamil M. tuberculosis Multidrug resistance protein 1 D 591 Hydrochloride Ca2+ channels metabolite (±)-Norverapamil D-591 Hydrochloride efflux D591 Hydrochloride Ca channels P-glycoprotein inhibit Norverapamil Hydrochloride ABCB1 Cluster of differentiation 243 (±)-Norverapamil hydrochloride D 591 pumps D591 hydrochloride D-591 D591 Pgp inhibitor

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