5.30151

ATGL Inhibitor, Atglistatin

• Sinonimo/i: ATGL Inhibitor, Atglistatin, 3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
• Formula empirica (notazione di Hill): C₁₇H₂₁N₃O
• Numero CAS: 1469924-27-3
• Peso molecolare: 283.37
• Numero MDL: MFCD28009494
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Stato: powder
• Potenza: 700 nM IC₅₀; 355 nM K_i
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; protect from light
• Colore: beige
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: 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); AWOPBSAJHCUSAS-UHFFFAOYSA-N

Descrizione

Descrizione generale

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 vitro and in blood of mice in vivo via 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.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
ATGL

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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

Produced under the license of University of Graz/Graz University of Technology

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable