ATGL Inhibitor, Atglistatin-Calbiochem

半岛bd体育手机客户端 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 ?M) in a substrate-competitive (K_i= 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 ?M. Shown to effectively suppress FA/glycerol productions from adipocytes (IC_max= 50 to 100 ?M in 3T3-L1-differentiated adipocytes or primary murine white adipose tissue/WAT cultures)in vitroand in blood of micein vivovia either oral or intraperitoneal administration (ED_max= 200 ?mol/kg) without affecting plasma glucose, total cholesterol, insulin, or β-hydroxybutyrate (beta-HB) level. Significant cytotoxicity is reported at concentrations >50 ?M 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 ?mol/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

半岛bd体育手机客户端 性质

质量水平	100
测定	≥97% (HPLC)
形式	powder
效能	700 nM IC50 355 nM Ki
manufacturer/tradename	Calbiochem?
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
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable