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- 详细信息
- 文献和实验
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
CM-4620
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1713240-67-5
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥2784.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥1173.0 |
| 规格: | 5 mg | 产品价格: | ¥3000.0 |
| 规格: | 10 mg | 产品价格: | ¥4713.0 |
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Zegocractin
CAS No. : 1713240-67-5
MCE 国际站:Zegocractin
产品活性: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。
研究领域:Membrane Transporter/Ion Channel
作用靶点:CRAC Channel
In Vitro: 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).
In Vivo: 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.
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