892711-75-0
892711-75-0 結(jié)構(gòu)式
基本信息
4-異丙氧基-N-(2-甲基喹啉-8-基)苯甲酰胺
4-isopropoxy-N-(2-methylquinolin-8-yl)benzamide
N-(2-methylquinolin-8-yl)-4-propan-2-yloxybenzamide
4-(1-Methylethoxy)-N-(2-methyl-8-quinolinyl)benzamide
Benzamide, 4-(1-methylethoxy)-N-(2-methyl-8-quinolinyl)-
Inhibitor,CDN 1163,Calcium Channel,Ca channels,Ca2+ channels,CDN-1163,CDN1163,inhibit
物理化學(xué)性質(zhì)
常見問題列表
| Target | Value |
|
SERCA
() |
CDN1163 (5.5-25?mM; 0-8 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: | 5.5?mM, 25?mM |
| Incubation Time: | 0 hour, 4 hours, 8 hours |
| Result: | High glucose-induced resistin and nuclear NFATc expression were 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 Ca 2+ -ATPase activity, decreases endoplasmic reticulum (ER) stress-induced cell death in vitro and improves liver Ca 2+ 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. |