CAS NO: | 1713240-67-5 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cas No. | 1713240-67-5 |
别名 | CM-4620 |
Canonical SMILES | O=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 tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation 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: |