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.
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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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