產品描述: | 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 |
靶點: |
Calcium channel blocker P-glycoprotein (P-gp) inhibitor;CalciumChannel;P-gp;DrugMetabolite |
體內研究: |
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 |
參考文獻: |
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. 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. 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 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. |
溶解性: |
H2O : ≥ 50 mg/mL (104.81 mM) DMSO : ≥ 31 mg/mL (64.98 mM) |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.096 ml |
10.481 ml |
20.963 ml |
5 mM |
0.419 ml |
2.096 ml |
4.193 ml |
10 mM |
0.21 ml |
1.048 ml |
2.096 ml |
50 mM |
0.042 ml |
0.21 ml |
0.419 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |