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Desmethyl Carvedilol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Desmethyl Carvedilol图片
CAS NO:72956-44-6
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
An active metabolite of carvedilol
Cas No.72956-44-6
别名O-去甲卡维地洛
Canonical SMILESOC1=C(OCCNCC(COC2=C(C(C=CC=C3)=C3N4)C4=CC=C2)O)C=CC=C1
分子式C23H24N2O4
分子量392.5
溶解度DMSO: soluble
储存条件-20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Desmethyl carvedilol is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist carvedilol .1,2,3It is formed from carvedilol by the cytochrome P450 (CYP) isoform CYP2C9.1Desmethyl carvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50= 7.62 µM), a mutation that results in spontaneous calcium release from the endoplasmic reticulum.2It reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by isoproterenol in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively).3

1.Oldham, H.G., and Clarke, S.E.In vitro identification of the human cytochrome P450 enzymes involved in the metabolism of R(+)- and S(-)-carvedilolDrug Metab. Dispos.25(8)970-977(1997) 2.Smith, C.D., Wang, A., Vembaiyan, K., et al.Novel carvedilol analogues that suppress store-overload-induced Ca2+ releaseJ. Med. Chem.56(21)8625-8655(2013) 3.Strein, K., Sponer, G., MÜller-Beckmann, B., et al.Pharmacological profile of carvedilol, a compound with β-blocking and vasodilating propertiesJ. Cardiovasc. Pharmacol.10(Suppl. 11)S33-S41(1987)