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ATGL Inhibitor, Atglistatin-Calbiochem

品牌
Sigma-Aldrich
货号
5.30151
规格纯度
A cell-permeable, selective inhibitor of adipose triglyceride lipase activity (IC50 = 700 nM).
参考价格
2289.97 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
ATGL Inhibitor, Atglistatin-Calbiochem
3-(4'-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
产品介绍:

产品说明

一般描述

A cell-permeable biphenyldimethyl urea compound that inhibits adipose triglyceride lipase (ATGL) activity (IC50 = 700 nM; [Substrate] = [Triolein] = 165 µM) in a substrate-competitive (Ki = 355 nM) and highly selective manner, exhibiting little potency against hormone-sensitive lipase (HSL), monoglyceride lipase (MGL), pancreatic lipase, lipoprotein lipase, or lysophospholipases PNPLA6/7 even at concentrations as high as 100 µM. Shown to effectively suppress FA/glycerol productions from adipocytes (ICmax = 50 to 100 µM in 3T3-L1-differentiated adipocytes or primary murine white adipose tissue/WAT cultures) in vitro and in blood of mice in vivo via either oral or intraperitoneal administration (EDmax = 200 µmol/kg) without affecting plasma glucose, total cholesterol, insulin, or β-hydroxybutyrate (beta-HB) level. Significant cytotoxicity is reported at concentrations >50 µM in AML-12 murine hepatocyte cultures. Although ATGL deficiency causes cardiomyopathy in human and ATGL-ko animals due to severe triacylglycerol (TG) accumulation in cardiac muscle, significant atglistatin level (>0.2 nmol/g tissue) is only seen in liver, white and brown adipose tissues, and detectable TG accumulation is only observed in liver tissue in wt mice 8 h post single 200 µmol/kg oral dosage.

生化/生理作用

Cell permeable: yes
Primary Target
ATGL
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Mayer, N., et al. 2013. Nat. Chem. Biol.9, 785.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C17H21N3O
分子量283.37

产品性质

质量水平100
测定≥97% (HPLC)
形式powder
效能700 nM IC50
355 nM Ki
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 beige
溶解性DMSO: 100 mg/mL
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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