| 产品描述: | CDN1163 is an allosteric sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) activator that improves Ca2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders |
| 靶点: |
SERCA;CalciumChannel |
| 体外研究: |
CDN1163 (10?μM; 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. |
| 体内研究: |
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. |
| 参考文献: |
1. Kang S, et al. Small Molecular Allosteric Activator of the Sarco/Endoplasmic Reticulum Ca2+-ATPase (SERCA) Attenuates Diabetes and Metabolic Disorders. J Biol Chem. 2016 Mar 4;291(10):5185-98. 2. Singh R, et al. A role for calcium in resistin transcriptional activation in diabetic hearts. Sci Rep. 2018 Oct 23;8(1):15633. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.121 ml |
15.606 ml |
31.212 ml |
| 5 mM |
0.624 ml |
3.121 ml |
6.242 ml |
| 10 mM |
0.312 ml |
1.561 ml |
3.121 ml |
| 50 mM |
0.062 ml |
0.312 ml |
0.624 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |