516567 Sigma-AldrichPPARβ/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.
More>> 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. Less<<Synonyms: 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
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Overview
Key Specifications Table
CAS # | Empirical Formula |
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188591-46-0 | C₁₅H₁₂ClF₃N₂O₃S |
Pricing & Availability
Catalog Number | Availability | Packaging | Qty/Pack | Price | Quantity | |
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516567-10MG |
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Glass bottle | 10 mg |
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Description | |
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Overview | A 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 Number | 516567 |
Brand Family | Calbiochem® |
Synonyms | 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I |
References | |
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References | Palkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419. Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857. |
Product Information | |
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CAS number | 188591-46-0 |
Form | White solid |
Hill Formula | C₁₅H₁₂ClF₃N₂O₃S |
Chemical formula | C₁₅H₁₂ClF₃N₂O₃S |
Structure formula Image | |
Quality Level | MQ100 |
Biological Information | |
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Purity | ≥99% by HPLC |
Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
Global Trade Item Number | |
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Catalog Number | GTIN |
516567-10MG | 04055977198201 |