Zegocractin

产品说明书

Print
Chemical Structure| 1713240-67-5 同义名 : CM-4620
CAS号 : 1713240-67-5
货号 : A605542
分子式 : C19H11ClF3N3O3
纯度 : 99%+
分子量 : 421.76
MDL号 : MFCD30489478
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • Calcium Channel

    Orai1/STIM1-mediated Ca2+ currents, IC50:120 nM

  • Calcium Channel

    Orai1/STIM1-mediated Ca2+ currents, IC50:120 nM
描述 CM-4620 is a CRAC (calcium-release activated calcium-channel) inhibitor with IC50 values of 119, 895 nM for Orai1/STIM1 and Orai2/STIM1 channels, respectively. Treatment with CM-4620 blocked SOCE in mouse pancreatic acinar cells in a dose-dependent manner, with IC50 value of 0.7μM, indicating that it may block the cell’s ability to reload its ER with Calcium for successive rounds of signaling. Also CCK-induced Ca2+ entry in mouse pancreatic acinar cells could blocked by CM-4620. Release of multiple cytokines, like IFNgamma, IL-4, IL-6, IL-1beta, IL-6, IL-10, TNF-alpha, IL-2 and IL-17, were potently inhibited by CM-4620. Intraperitoneal injection with CM-4620 at dose ranging in 2-20mg/kg produced significant and dose-dependent reductions in caerulein-induced pathology in the mouse pancreas.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.71mL

4.74mL

2.37mL