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892711-75-0

中文名稱(chēng) 4-異丙氧基-N-(2-甲基喹啉-8-基)苯甲酰胺
英文名稱(chēng) CDN 1163
CAS 892711-75-0
分子式 C20H20N2O2
分子量 320.39
MOL 文件 892711-75-0.mol
更新日期 2023/03/20 15:41:25
892711-75-0 結(jié)構(gòu)式 892711-75-0 結(jié)構(gòu)式

基本信息

中文別名
化合物CDN1163
4-異丙氧基-N-(2-甲基喹啉-8-基)苯甲酰胺
英文別名
CDN1163
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
所屬類(lèi)別
生物化工:生化試劑

物理化學(xué)性質(zhì)

熔點(diǎn)87 - 89°C
儲(chǔ)存條件2-8°C
溶解度溶于DMSO(>25mg/ml)
形態(tài)粉末
顏色白色至米色
穩(wěn)定性Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338

常見(jiàn)問(wèn)題列表

生物活性
CDN1163是一種 sarco/endoplasmic reticulum Ca2+-ATPase (SERCA) 的小分子變構(gòu)激活劑,可改善 Ca2+ 穩(wěn)態(tài)。
靶點(diǎn)
TargetValue
SERCA
()
體外研究

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.
體內(nèi)研究

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.
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