530151 ATGL Inhibitor, Atglistatin - Calbiochem

530151
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₇H₂₁N₃O

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.30151.0001
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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
          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.