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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.

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Sinónimos: 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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CAS #Empirical Formula
188591-46-0C₁₅H₁₂ClF₃N₂O₃S

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516567-10MG
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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
      Biological Information
      Purity≥99% by HPLC
      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
      Global Trade Item Number
      Número de referencia GTIN
      516567-10MG 04055977198201