您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > GNE-131
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
GNE-131
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。
GNE-131图片
CAS NO:1629063-81-5
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
GNE-131是人类钠离子通道NaV1.7(hNaV1.7)有效的、选择性抑制剂，其IC50值为3nM。
Cas No.1629063-81-5
Canonical SMILESO=S(NC1=NN=C2N1C=C(C3CC3)C(OCC45C[C@@H](C6)C[C@@H](C[C@@H]6C5)C4)=C2)(C7CC7)=O
分子式C23H30N4O3S
分子量442.57
溶解度DMSO : 125 mg/mL (282.44 mM)
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

GNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.

GNE-131 (Compound 13) shows moderate clearance in human liver microsomes and excellent functional activity against human NaV1.7 with an IC50 of 0.003±0.001 μM. GNE-131 shows excellent potency, good in vitro metabolic stability[1].

GNE-131 shows low in vivo clearance in mouse, rat, and dog. GNE-131 also displays excellent efficacy in a transgenic mouse model of induced pain[1].

[1]. Focken T, et al. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 Jun 14;61(11):4810-4831.