A-922500
- A 922500;DGAT-1 Inhibitor 4a
货号: abs813326
货号-规格 | 货期 | 价格 | 数量 |
abs813326-5mg | 1-2周 | ¥1325.00 | - + |
abs813326-10mg | 1-2周 | ¥1877.00 | - + |
abs813326-50mg | 1-2周 | ¥5989.00 | - + |

产品描述 | |
描述 | A-922500是人类和小鼠DGAT-1抑制剂,IC50分别为7 nM和24 nM,比作用于相关的酰基转移酶,hERG及抗靶面板的选择性高。 |
纯度 | >98% |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
基本信息 | |
别名 | A 922500;DGAT-1 Inhibitor 4a |
可溶性/溶解性 | DMSO :21.4 mg/mL (50 mM) |
生物活性 | |
靶点 | human DGAT-1 ,mouse DGAT-1 |
In vitro(体外研究) | A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1. |
In vivo(体内研究) | Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. |
参考文献 | |
参考文献 |