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

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

Cat. No.: HY-100750 Purity: 98.26%
Handling Instructions

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

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

Norverapamil hydrochloride Chemical Structure

Norverapamil hydrochloride Chemical Structure

CAS No. : 67812-42-4

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10 mM * 1 mL in DMSO USD 151 In-stock
Estimated Time of Arrival: December 31
2 mg USD 96 In-stock
Estimated Time of Arrival: December 31
5 mg USD 144 In-stock
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10 mg USD 252 In-stock
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25 mg USD 564 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Norverapamil hydrochloride:

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Description

Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), 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

Calcium channel blocker[1]
P-glycoprotein (P-gp) inhibitor[2]

In Vitro

Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) 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].

In Vivo

Norverapamil hydrochloride (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].

Animal Model: Male Sprague-Dawley rats[3]
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

477.04

Formula

C₂₆H₃₇ClN₂O₄

CAS No.

67812-42-4

SMILES

N#CC(C(C)C)(CCCNCCC1=CC=C(OC)C(OC)=C1)C2=CC=C(OC)C(OC)=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

H2O : ≥ 50 mg/mL (104.81 mM)

DMSO : ≥ 31 mg/mL (64.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0963 mL 10.4813 mL 20.9626 mL
5 mM 0.4193 mL 2.0963 mL 4.1925 mL
10 mM 0.2096 mL 1.0481 mL 2.0963 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Norverapamil(±)-NorverapamilD591D 591D-591Calcium ChannelP-glycoproteinDrug MetaboliteCa2+ channelsCa channelsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243metabolitemycobacterialeffluxpumpsM. tuberculosisInhibitorinhibitorinhibit

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Product name:
Norverapamil hydrochloride
Cat. No.:
HY-100750
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