CM-4620 是一种钙离子释放激活通道的抑制剂，对Orai1/STIM1和Orai2/STIM1的IC50值分别为 119 和 895 nM。

CM4620 is a calcium-release activated calcium-channel (CRAC channel) inhibitor.

CM-4620 (compound 1) 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-6: 135 nM, IL-4: 879 nM, IL-1β: 240 nM, IL-10: 303 nM, IL-2: 59 nM, TNFα: 225 nM, IL-17 120 nM) [1].

Mouse PACs are treated with CRAC inhibitors GSK-7975A or CM-4620 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 control levels upon treatment with 700 nM of inhibitor. CM-4620 blocks 100% of the reuptake at 10 mM.

1713240-67-5

C19H11ClF3N3O3

421.76

N-(5-(6-Chloro-2,2-difluorobenzo[d][1,3]dioxol-5-yl)pyrazin-2-yl)-2-fluoro-6-methylbenzamide;CM4620;CM-4620

H2O:Insoluble
DMSO:100 mg/mL (237.10 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years