516567 PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem

516567
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₅H₁₂ClF₃N₂O₃S 188591-46-0

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      516567-10MG
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable pyridylsulfone that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC50 = 126 nM in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium; 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
          Catalogue Number516567
          Brand Family Calbiochem®
          Synonyms4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
          References
          ReferencesPalkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
          Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.
          Product Information
          CAS number188591-46-0
          FormWhite solid
          Hill FormulaC₁₅H₁₂ClF₃N₂O₃S
          Chemical formulaC₁₅H₁₂ClF₃N₂O₃S
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥99% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          Certificates of Analysis

          TitleLot Number
          516567

          References

          Reference overview
          Palkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
          Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.
          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.

          Revision02-October-2012 JSW
          Synonyms4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
          DescriptionA cell-permeable and orally available pyridylsulfone compound that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC50 = 126 nM against 2 nM GW501516-induced reporter transcription in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium by 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number188591-46-0
          Chemical formulaC₁₅H₁₂ClF₃N₂O₃S
          Structure formulaStructure formula
          Purity≥99% by HPLC
          SolubilityDMSO (50 mg/ml; clear, colorless solution)
          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
          ReferencesPalkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
          Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.