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ICA 069673
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。
ICA 069673图片
CAS NO:582323-16-8
包装:50mg
市场价:4967元

产品介绍
ICA 069673 是一种 KCNQ2/Q3 钾通道激活剂,IC50 为 0.69 μM。
Cas No.582323-16-8
化学名(Z)-N-(2-chloropyrimidin-5-yl)-3,4-difluorobenzimidic acid
Canonical SMILESClC1=NC=C(/N=C(O)/C2=CC(F)=C(F)C=C2)C=N1
分子式C11H6ClF2N3O
分子量269.63
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 30 mg/ml
储存条件Store at RT
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

ICA-069673 is a KCNQ2/Q3 potassium channel activator with an IC50 of 0.69 μM.

ICA-069673 is found to be 20-fold selective for KCNQ2/Q3 over KCNQ3/Q5 and has no measurable activity against a panel of cardiac ion channels (IC50 values >30 μM for hERG, Nav1.5, L type channels, and KCNQ1) as well as no activity on GABA(A) gated channels at 10 μM[1]. ICA-069673 exhibits much stronger effects on KCNQ2 channels, including a large hyperpolarizing shift of the voltage-dependence of activation, an 2-fold enhancement of peak current and pronounced subtype specificity for KCNQ2 over KCNQ3. Based on ICA73 sensitivity of chimeric constructs of the transmembrane segments of KCNQ2 and KCNQ3, this drug appears to interact with the KCNQ2 voltage sensor (S1-S4)[2].

References:
[1]. Wickenden AD, et al. N-(6-chloro-pyridin-3-yl)-3,4-difluoro-benzamide (ICA-27243): a novel, selective KCNQ2/Q3 potassium channel activator. Mol Pharmacol. 2008 Mar;73(3):977-86. Epub 2007 Dec 18.
[2]. Wang AW, et al. Sequence determinants of subtype-specific actions of KCNQ channel openers. J Physiol. 2017 Feb 1;595(3):663-676.