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Norverapamil hydrochloride

Cat. No. M14203
Norverapamil hydrochloride Structure
Synonym:

(±)-Norverapamil hydrochloride; D591 hydrochloride

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Biological Activity

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.

Chemical Information
Molecular Weight 477.04
CAS Number 67812-42-4
Solubility (25°C) Water ≥ 50 mg/mL
DMSO ≥ 31 mg/mL
Storage 2-8°C, protect from light, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shuangjiao Sun, et al. Determination of Verapamil Hydrochloride and Norverapamil Hydrochloride in Rat Plasma by Capillary Electrophoresis With End-Column Electrochemiluminescence Detection and Their Pharmacokinetics Study

[2] Azadeh Haeri, et al. Metabolite parameters as an appropriate alternative approach for assessment of bioequivalence of two verapamil formulations

[3] Fabiano Henrique Mateus, et al. Simultaneous analysis of the enantiomers of verapamil and norverapamil in rat plasma by liquid chromatography-tandem mass spectrometry

[4] D R Abernethy, et al. Verapamil and norverapamil determination in human plasma by gas-liquid chromatography using nitrogen-phosphorus detection: application to single-dose pharmacokinetic studies

[5] G D Kozloski, et al. Bioequivalence of verapamil hydrochloride extended-release pellet-filled capsules when opened and sprinkled on food and when swallowed intact

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  Catalog
Abmole Inhibitor Catalog




Keywords: Norverapamil hydrochloride, (±)-Norverapamil hydrochloride; D591 hydrochloride supplier, Calcium Channel, inhibitors, activators


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