生物活性 | |||
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描述 | The sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) pumps Ca2+ from the cytoplasm into the endoplasmic reticulum (ER). CDN1163 is a small-molecule allosteric activator of SERCA that acts directly on SERCA and improves Ca2+ homeostasis. CDN1163 at 1 – 11μM dose-dependently increased the Vmax of SERCA2 Ca2+-ATPase activity in the ER microsomes from liver tissues. CDN1163 at 10μM rescued cells from H2O2-stimulated cell death. In ob/ob male mice, intraperitoneal injection with 300μL of CDN1163 (50mg/kg/day) for 5 days reduced blood glucose levels and improved metabolic parameters compared with the vehicle-treated group. Treatment with CDN1163 also resulted in a 16% decrease in adipose tissue weight, reduced gluconeogenic gene expression, reversed hepatic steatosis, and inhibited ER stress and ER stress-induced apoptosis in ob/ob mice[3]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.12mL 0.62mL 0.31mL |
15.61mL 3.12mL 1.56mL |
31.21mL 6.24mL 3.12mL |
参考文献 |
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