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Vanoxerine dihydrochloride
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。
Vanoxerine dihydrochloride图片
CAS NO:67469-78-7
包装与价格：
包装价格(元)
10mg电议
25mg电议
50mg电议

产品介绍
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) 是一种竞争性、有效和高度选择性的多巴胺再摄取抑制剂 (Ki=1 nM)。
Cas No.67469-78-7
别名伐诺司林二盐酸盐,GBR-12909 dihydrochloride; I893 dihydrochloride
化学名1-(2-(bis(4-fluorophenyl)methoxy)ethyl)-4-(3-phenylpropyl)piperazine dihydrochloride
Canonical SMILESFC1=CC=C(C(OCCN2CCN(CC2)CCCC3=CC=CC=C3)C4=CC=C(F)C=C4)C=C1.Cl.Cl
分子式C28H34Cl2F2N2O
分子量523.49
溶解度DMF: 2 mg/ml,DMSO: 2 mg/ml
储存条件Store at -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

Vanoxerine is an antagonist of dopamine transporter (DAT1) with Ki value of 16.9nM [1].

As an antagonist of DAT, vanoxerine is developed for treatment of Parkinson's disease and depression but has no effect on these diseases. Vanoxerine is also found to have desirable cardiac antiarrhythmic properties. It is a blocker of cardiac hERG (hKv11.1) with IC50 value of 0.84nM. It also blocks the ICa,L and hNav1.5 channel with IC50 values of 320nM and 830nM, respectively. Vanoxerine does not significantly prolong Purkinje fiber APD60 and APD90 and has no significant effect on QT or TDR. Further, the clinical trial demonstrates that the effective concentrations of vanoxerine are well tolerated and safe in man [2].

References:
[1] Giros B, el Mestikawy S, Godinot N, Zheng K, Han H, Yang-Feng T, Caron MG. Cloning, pharmacological characterization, and chromosome assignment of the human dopamine transporter. Mol Pharmacol. 1992 Sep;42(3):383-90.
[2] Lacerda AE, Kuryshev YA, Yan GX, Waldo AL, Brown AM. Vanoxerine: cellular mechanism of a new antiarrhythmic. J Cardiovasc Electrophysiol. 2010 Mar;21(3):301-10.