Norverapamil
Based on 2 publication(s) in Google Scholar
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Norverapamil hydrochloride) usually boasts enhanced water solubility and stability.
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- CAS No.: 67018-85-3
- Formule: C26H36N2O4
- Masse moléculaire:440.58
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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HY-14275
VerapamilCalcium Channel Blocker -
HY-14275R
Verapamil (Standard)Calcium Channel Blocker -
HY-100750
Norverapamil hydrochlorideL-type Calcium Channel Blocker -
HY-136589
Verapamil EP Impurity C hydrochlorideCytochrome P450 Inhibitor -
HY-100750R
Norverapamil hydrochloride (Standard)L-type Calcium Channel Blocker
Publications Citing Use of MedChemExpress (MCE) Norverapamil
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Activité biologique
Description
IC50 & Target
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L-type calcium channel |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Caco-2 | IC50 |
0.3 μM
Compound: Norverapamil
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells
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[PMID: 10773005] |
| NIH-3T3-G185 | IC50 |
0.9 μM
Compound: Norverapamil
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TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
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[PMID: 11743742] |
In Vitro
Norverapamil ((±)-Norverapamil) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil[1].
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 clinic[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats[4]
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Dosage:9 mg/kg (Pharmacokinetic Study)
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Administration:Oral administration
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Result:t1/2=9.4 hours; AUC=260 ng▪h/mL; Cmax=41.6 ng/mL.
Chemical Information
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CAS No. 67018-85-3
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Masse moléculaire 440.58
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Formule C26H36N2O4
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SMILES
N#CC(C(C)C)(CCCNCCC1=CC=C(OC)C(OC)=C1)C2=CC=C(OC)C(OC)=C2
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Synonyms
(±)-Norverapamil; D591
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Biochem Pharmacol
BMAL1-mediated transcriptional regulation of CYP3A13 drives circadian rhythms in intestinal first-pass metabolism. [Abstract]2026 Apr 16;250(Pt 1):117981. PMID: 42000077 -
Toxicol Lett
Lactobacillus rhamnosus induces CYP3A and changes the pharmacokinetics of verapamil in rats. [Abstract]2021 Nov 1:352:46-53. PMID: 34600097
Pureté et documentation
Références
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Norverapamil Related Classifications
HY-135328 Related Classifications
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Keywords
- Norverapamil
- 67018-85-3
- (±)-Norverapamil
- D591
- D591
- D 591
- D-591
- Calcium Channel
- P-glycoprotein
- Drug Metabolite
- Ca2+ channels
- Ca channels
- P-gp
- Pgp
- Multidrug resistance protein 1
- MDR1
- ATP-binding cassette sub-family B member 1
- ABCB1
- Cluster of differentiation 243
- CD243
- metabolite
- mycobacterial
- efflux
- pumps
- M. tuberculosis
- Inhibitor
- inhibitor
- inhibit