5.30151

ATGL Inhibitor, Atglistatin

• 동의어(들): ATGL Inhibitor, Atglistatin, 3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
• 실험식(Hill 표기법): C₁₇H₂₁N₃O
• CAS Number: 1469924-27-3
• Molecular Weight: 283.37
• UNSPSC 코드: 51111800
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 형태: powder
• 효능: 700 nM IC₅₀; 355 nM K_i
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: beige
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
ATGL

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable