| 产品描述: | Zegocractin (CM-4620) 是一种钙离子释放激活通道 (CRAC channel) 的抑制剂,其对 Orai1/STIM1 和 Orai2/STIM1 的 IC50 值分别为 119 nM 和 895 nM。 |
| 靶点: |
IC50: 119 nM (Orai 1/STIM1), 895 nM (Orai 1/STIM1) |
| 体外研究: |
It is determined that Zegocractin (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, Zegocractin 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). |
| 体内研究: |
Mouse PACs are treated with CRAC inhibitors Zegocractin 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. Zegocractin blocks 100% of reuptake at 10 mM. |
| 参考文献: |
1. ARYL SULFONOHYDRAZIDES. WO2016/138472Al. |
| 溶解性: |
soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.371 ml |
11.855 ml |
23.71 ml |
| 5 mM |
0.474 ml |
2.371 ml |
4.742 ml |
| 10 mM |
0.237 ml |
1.186 ml |
2.371 ml |
| 50 mM |
0.047 ml |
0.237 ml |
0.474 ml |
|
| 注意: |
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