516567

PPARβ/δ Antagonist, GSK3787

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.

• Synonyme(s) : PPARβ/δ Antagonist, GSK3787, 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl)sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
• Formule empirique (notation de Hill): C₁₅H₁₂ClF₃N₂O₃S
• Numéro CAS: 188591-46-0
• Poids moléculaire : 392.78
• Numéro MDL: MFCD00099612
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥99% (HPLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: white
• Solubilité: DMSO: 50 mg/mL, clear, colorless
• Conditions d'expédition: ambient
• Température de stockage: 2-8°C
• InChI: 1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)
• Clé InChI: JFUIMTGOQCQTPF-UHFFFAOYSA-N

Description

Description générale

A 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).

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).

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Palkar, P.S., et al. 2010. Mol. Pharmacol.78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem.53, 1857.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable