5.30151
Atglistatin
≥97% (HPLC), adipose triglyceride lipase (ATGL) inhibitor, powder
Synonym(s):
ATGL Inhibitor, Atglistatin, 3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
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| Size/SKU | Availability | Price |
|---|---|---|
10 mg | Please contact Customer Service for Availability | $311.00 |
About This Item
Empirical Formula (Hill Notation):
C17H21N3O
CAS Number:
Molecular Weight:
283.37
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
Assay:
≥97% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
Product Name
ATGL Inhibitor, Atglistatin,
assay
≥97% (HPLC)
Quality Segment
form
powder
potency
700 nM IC50, 355 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
beige
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
SMILES string
N(C)(C)c1ccc(cc1)c2cc(ccc2)NC(=O)N(C)C
InChI
1S/C17H21N3O/c1-19(2)16-10-8-13(9-11-16)14-6-5-7-15(12-14)18-17(21)20(3)4/h5-12H,1-4H3,(H,18,21)
InChI key
AWOPBSAJHCUSAS-UHFFFAOYSA-N
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 (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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
ATGL
ATGL
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
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 Technology
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
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Storage Class
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
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