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530151 ATGL Inhibitor, Atglistatin - Calbiochem

530151
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₇H₂₁N₃O

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      Glass bottle 10 mg
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      Description
      OverviewA 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. Shown to effectively suppress FA/glycerol productions from adipocytes (ICmax = 50 to 100 µM in 3T3-L1-differentiated adipocytes or primary murine WAT cultures) in vitro and in blood of mice in vivo via either oral or intraperitoneal administration (EDmax = 200 µmol/kg) with no significant cytotoxicity up to 50 µM in AML-12 murine hepatocyte cultures. Although TG accumulation in cardiac muscle causes cardiomyopathy, significant Atglistatin level is only seen in liver, white & brown adipose tissues in wt mice 8 h post single 200 µmol/kg oral dosage.
      Catalogue Number530151
      Brand Family Calbiochem®
      Synonyms3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
      References
      ReferencesMayer, N., et al. 2013. Nat. Chem. Biol. 9, 785.
      Product Information
      FormBeige powder
      Hill FormulaC₁₇H₂₁N₃O
      Chemical formulaC₁₇H₂₁N₃O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetATGL
      Primary Target IC<sub>50</sub>700 nM
      Primary Target K<sub>i</sub>355 nM)
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      ATGL Inhibitor, Atglistatin - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Mayer, N., et al. 2013. Nat. Chem. Biol. 9, 785.
      Data Sheet

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision29-April-2014 JSW
      Synonyms3-(4ʹ-(Dimethylamino)biphenyl-3-yl)-1,1-dimethylurea, Adipose Triglyceride Lipase Inhibitor
      DescriptionA 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 in vitro and in blood of mice in vivo via either oral or intraperitoneal administration (EDmax50 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 & 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.
      FormBeige powder
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₇H₂₁N₃O
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage +2°C to +8°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Standard Handling
      ReferencesMayer, N., et al. 2013. Nat. Chem. Biol. 9, 785.