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<<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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Overview
Key Spec Table
| CAS # | Empirical Formula |
|---|---|
| 188591-46-0 | C₁₅H₁₂ClF₃N₂O₃S |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 516567-10MG | Glass bottle | 10 mg |
| Description | |
|---|---|
| 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 | |
|---|---|
| References | Palkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419. Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857. |
| Product Information | |
|---|---|
| CAS number | 188591-46-0 |
| Form | White solid |
| Hill Formula | C₁₅H₁₂ClF₃N₂O₃S |
| Chemical formula | C₁₅H₁₂ClF₃N₂O₃S |
| Structure formula Image | |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Purity | ≥99% by HPLC |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 516567-10MG | 04055977198201 |