CM-4620 (Synonyms: CM-4620) |
| カタログ番号GC19107 |
CM-4620（CM-4620）は、カルシウム放出活性化カルシウムチャネル（CRACチャネル）阻害剤であり、Orai1 / STIM1およびOrai2 / STIM1チャネルに対するIC50はそれぞれ119 nMおよび895 nMです。
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Cas No.: 1713240-67-5
Sample solution is provided at 25 µL, 10mM.
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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.
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