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

The PPARβ/δAntagonist II, PT-S58, also referenced under CAS 188591-46-0, controls the biological activity of PPARβ/δ. This small molecule/inhibitor is primarily used for Biochemicals applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I

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516567
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
188591-46-0C₁₅H₁₂ClF₃N₂O₃S

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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
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalogue Number GTIN
      516567-10MG 04055977198201

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem 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 Protect from light
      +2°C to +8°C
      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.