1. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  2. Calcium Channel P-glycoprotein Drug Metabolite
  3. Norverapamil

Norverapamil  (Synonyms: (±)-Norverapamil; D591)

Cat. No.: HY-135328
Handling Instructions

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.

For research use only. We do not sell to patients.

Norverapamil Chemical Structure

Norverapamil Chemical Structure

CAS No. : 67018-85-3

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Description

Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2].

IC50 & Target

L-type calcium channel

 

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

Norverapamil (9 mg/kg; p.o.), a major metabolite of verapamil, has terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng▪h/ml, and 41.6 ng/mL, respectively[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats[4]
Dosage: 9 mg/kg (Pharmacokinetic Study)
Administration: Oral administration
Result: t1/2=9.4 hours; AUC=260 ng▪h/mL; Cmax=41.6 ng/mL.
Molecular Weight

440.58

Formula

C26H36N2O4

CAS No.
SMILES

N#CC(C(C)C)(CCCNCCC1=CC=C(OC)C(OC)=C1)C2=CC=C(OC)C(OC)=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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