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.

Information

A922500 A922500 (DGAT-1 Inhibitor 4a) is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
In vitro

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

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.
Cell Data

cell lines：HUVECs

Concentrations：

Incubation Time：

Powder Purity:≥99%

规格

英文别名

DGAT-1 Inhibitor 4a | Cyclopentanecarboxylic acid, 2-[[4'-[[(phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]-, (1R,2R)-

规格或纯度

10mM in DMSO

英文名称

A922500

生化机理

A922500 （DGAT-1 抑制剂 4a）是人和小鼠 DGAT-1 的抑制剂，其 IC50 值分别为 7 nM 和 24 nM，对相关酰基转移酶、hERG 和一系列抗靶标具有良好的选择性。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

名称和识别符

EC号

688-540-9

分子类型

小分子

Isomeric SMILES

C1C[C@H]([C@@H](C1)C(=O)O)C(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)NC(=O)NC4=CC=CC=C4

分子量

428.48

Reaxy-Rn

29788907

Reaxys-RN link address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=29788907&ln=

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关联靶点（人）

DGAT1 Tclin 二酰甘油O-酰基转移酶1(Diacylglycerol O-acyltransferase 1) (4 活性数据)

点击查看靶蛋白信息： DGAT1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

化学和物理性质

溶解性

Solubility (25°C) In vitro DMSO: 15 mg/mL (18.96 mM); Water: Insoluble; Ethanol: Insoluble;

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信号词

危险

危险声明

H301: 吞咽会中毒

H319: 引起严重眼睛刺激

H410: 对水生生物有剧毒并具有长期持续影响

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