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<<SDB (Sicherheitsdatenblätter), Analysenzertifikate und Qualitätszertifikate, Dossiers, Broschüren und andere verfügbare Dokumente.
Synonyme: 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
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Übersicht
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Key Spec Table
| CAS # | Empirical Formula |
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| 188591-46-0 | C₁₅H₁₂ClF₃N₂O₃S |
Preis & Verfügbarkeit
| Bestellnummer | Verfügbarkeit | Verpackung | St./Pkg. | Preis | Menge | |
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| 516567-10MG |
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Glasflasche | 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 |
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| Quality Level | MQ100 |
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| Purity | ≥99% by HPLC |
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| Packaging Information | |
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| Packaged under inert gas | Packaged under inert gas |
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| Specifications |
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| Global Trade Item Number | |
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| Bestellnummer | GTIN |
| 516567-10MG | 04055977198201 |
Documentation
PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem SDB
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PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem Analysenzertifikate
| Titel | Chargennummer |
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| 516567 |
Literatur
| Übersicht |
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| Palkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419. Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857. |
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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.
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