【产品介绍】：

产品介绍：DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol.产品用途：A922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages. 属性 产品名称 A922500 产品名称 A922500 别名 DGAT-1 Inhibitor 4a；(1R,2R)-2-[[4-[[(苯基氨基)羰基]氨基][1,1-联苯]-4-基]甲酰基]环戊烷羧酸 英文别名 (1R,2R)-2-[4-[4-(phenylcarbamoylamino)phenyl]benzoyl]cyclopentane-1-carboxylic acid；DGAT-1 Inhibitor 4a；(1R,2R)-2-[[4'-[[Phenylamino)carbonyl]amino] [1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid CAS编号 959122-11-3 分子式 C26H24N2O4 分子量 428.48 PubChem CID 24768261 规格或纯度 98% 生化机理 二酰基甘油酰基转移酶1（DGAT-1）抑制剂（在人和小鼠DGAT-1处的IC50值分别为7和24 nM），对DGAT-2，ACAT1或ACAT2没有活性。在不改变食物摄入量的情况下引起明显的体重减轻，并降低体内肝脏和血浆甘油三酸酯的水平。口服有效。 溶解性 溶于DMSO, 最高浓度 (mg/mL): 21.42, 最高浓度(mM): 50 储存温度 -20°C储存 运输条件 超低温冰袋运输 Delta生物试剂