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ICA 121431
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 121431图片
CAS NO:313254-51-2
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
ICA 121431 是一种纳摩尔强效和广谱电压门控钠通道 (Nav) 阻滞剂，对人 Nav1.1 和 Nav1.3 亚型显示等效选择性，IC50 值分别为 13 nM 和 23 nM。
Cas No.313254-51-2
化学名2,2-diphenyl-N-(4-(N-(thiazol-2-yl)sulfamoyl)phenyl)acetamide
Canonical SMILESO=C(NC1=CC=C(S(NC2=NC=CS2)(=O)=O)C=C1)C(C3=CC=CC=C3)C4=CC=CC=C4
分子式C23H19N3O3S2
分子量449.55
溶解度DMF: 15 mg/ml,DMSO: 15 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 0.1 mg/ml
储存条件Store at -20℃
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-121431 is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, but no inhibition on human, monkey and dog Nav1.7.IC50 value: 19 nM (rat Nav1.7) [1]Target: rat Nav1.7 inhibitorICA-121431 exhibited a spectrum of inhibitory activity for Nav human channel subtypes; equipotent inhibition of Nav1.3 and Nav1.1, less potent inhibition of Nav1.2, and much weaker inhibition of Nav1.7, Nav1.6, Nav1.4, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 μM). the unique subtype selective Nav channel inhibitors ICA-121431 and PF-04856264 interact with amino acid residues on an extracellular facing region of the homologous Domain 4 voltage sensor of Nav1.3 or Nav1.7, which is distinct from previously described interaction sites for TTX or local anesthetic-like Nav channel inhibitors.

References:
[1]. McCormack K, et al. Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels. Proc Natl Acad Sci U S A. 2013 Jul 16;110(29):E2724-32.