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CM-4620
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。
CM-4620图片
CAS NO:1713240-67-5
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

产品介绍
CM-4620 (CM-4620) 是一种钙释放激活的钙通道(CRAC 通道)抑制剂,对 Orai1/STIM1 和 Orai2/STIM1 通道的 IC50 分别为 119 nM 和 895 nM。
Cas No.1713240-67-5
别名CM-4620
Canonical SMILESO=C(NC1=NC=C(C2=C(Cl)C=C(OC(F)(F)O3)C3=C2)N=C1)C4=C(C)C=CC=C4F
分子式C19H11ClF3N3O3
分子量421.76
溶解度DMSO : ≥ 100 mg/mL (237.10 mM);Water :< 0.1 mg/mL (insoluble)
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

CM-4620 is a calcium-release activated calcium-channel (CRAC) inhibitor, with IC50s of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively.

It is determined that CM-4620 (compound 1) inhibits Orai 1/STIM1 channels with an IC50 of 119 nM, and Orai2/STIM1 channels with an IC50 of 895 nM. It is more potent on Orai1 than Orai2-type CRAC channels. In human PBMCs, CM-4620 potently inhibits release of multiple cytokines which play important roles in T cells (IC50s, IFN γ: 138 nM, IL-4: 879 nM, IL-6: 135 nM, IL-1β: 240 nM, IL-10: 303 nM, TNFα: 225 nM, IL-2: 59 nM, IL-17 120 nM)[1].

Mouse PACs are treated with CRAC inhibitors CM-4620 or GSK-7975A and monitored for their rate of Calcium uptake. Both CRAC inhibitors reduce the rate of store-operated Calcium entry into the ER to 50% of controllevels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of reuptake at 10 mM[1].

References:
[1]. ARYL SULFONOHYDRAZIDES. WO2016/138472Al.