CDN1163

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CDN1163 (CDN-1163) 是 SERCA2 的小分子变构激活剂。

CDN1163 (CDN-1163) is a small molecule, allosteric activator of SERCA2, dose-dependently increases the Vmax of SERCA2 Ca2+-ATPase activity in ER microsomes; increases Ca2+-ATPase activity and significantly enhances Ca2+ uptake into the ER, attenuates H2O2-stimulated cell death in HEK cells; improves glucose homeostasis and metabolic parameters, increases glucose tolerance in ob/ob mice; CDN1163 reduces lipid accumulation and decreases lipogenesis in obese mice livers.

CDN1163 (10μM; 24 hours; rat cardiac myocyte cells) treatment reduces high glucose-induced resistin and nuclear NFATc expression and increases the phosphorylation of AMPKα in a time-dependent manner. Western Blot Analysis Cell Line:Rat cardiac myocyte cells (H9c2)Concentration:10?μM Incubation Time:24 hours Result:High glucose-induced resistin and nuclear NFATc expression are significantly reduced. The phosphorylation of AMPKα is increased in a time-dependent manner.

CDN1163 (50 mg/kg; intraperitoneal injection; for 5 days; male ob/ob mice and lean ob/+ mice) increases SERCA2 Ca2+-ATPase activity, decreases endoplasmic reticulum (ER) stress-induced cell death in vitro and improves liver Ca2+ transport activity. CDN1163 reduces blood glucose levels and improves metabolic parameters and gluconeogenic gene expression, reverses hepatic steatosis, inhibits ER stress and ER stress-induced apoptosis, and improves mitochondrial efficiency in ob/ob mice in vivo. Animal Model:Male 8-10-week old ob/ob mice and lean ob/+ mice Dosage:50 mg/kg Administration:Intraperitoneal injection; for 5 days Result:Markedly lowered fasting blood glucose, improved glucose tolerance, and ameliorated hepatosteatosis but did not alter glucose levels or body weight. Increased expression of uncoupling protein 1 (UCP1) and UCP3 in brown adipose tissue and reduced the hepatic expression of genes involved in gluconeogenesis and lipogenesis, attenuated ER stress response and ER stress-induced apoptosis, and improved mitochondrial biogenesis, possibly through SERCA2-mediated activation of AMP-activated protein kinase pathway.

CDN 1163 | CDN-1163

GPCR/G Protein

Calcium Channel

Calcium Channel

——

——

892711-75-0

320.392

C20H20N2O2

>98% (HPLC)

DMSO : 50 mg/mL 156.06 mM; H2O : < 0.1 mg/mL

O=C(NC1=C2N=C(C)C=CC2=CC=C1)C3=CC=C(OC(C)C)C=C3

4-(1-Methylethoxy)-N-(2-methyl-8-quinolinyl)benzamide

(-20℃)

With Ice Pack

≥ 2 years