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.
Zegocractin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Pancreatic macrophages
70 nM, 200 nM, 600 nM
20 minutes
To study the effect of SARS-CoV-2 S1 protein on calcium signaling in pancreatic macrophages. Results showed that S1 induced Ca2+ signals in 33% of macrophages at 70 nM and in all cells at 600 nM.
Function (Oxf). 2022 Jan 31;3(2):zqac002
Pancreatic stellate cells
70 nM, 200 nM, 600 nM
20 minutes
To study the effect of SARS-CoV-2 S1 protein on calcium signaling in pancreatic stellate cells. Results showed that S1 induced Ca2+ signals in 25% of stellate cells at 70 nM and in all cells at 600 nM.
Function (Oxf). 2022 Jan 31;3(2):zqac002
Zegocractin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Spared nerve injury (SNI) model
Oral gavage
10 mg/kg
Once daily for 7 days
Evaluated the effect of Orai1 inhibitor CM4620 on neuropathic pain, found that CM4620 significantly mitigated mechanical allodynia in male mice
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