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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 | |||
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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 |