Sigma-Aldrich Atgl Inhibitor Atglistatin

Assay

≥97% (HPLC)

Quality Level

100

Form

powder

Potency

700 nM IC₅₀
355 nM K_i

Manufacturer/Tradename

Calbiochem^®

Storage Condition

OK to freeze
protect from light

Color

beige

Solubility

DMSO: 100 mg/mL

Storage Temp.

2-8°C

General Description

A cell-permeable biphenyldimethyl urea compound that inhibits adipose triglyceride lipase (ATGL) activity (IC₅₀= 700 nM; [Substrate] = [Triolein] = 165 µM) 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 µM. Shown to effectively suppress FA/glycerol productions from adipocytes (IC_max= 50 to 100 µM 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 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.

Biochem/Physiol Actions

Cell permeable: yesPrimary Target
ATGLReversible: yes

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

Mayer, N., et Al. 2013.Nat. Chem. Biol. 9,785.Produced under the license of University of Graz/Graz University of TechnologyCALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany