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.

• 別名: PPARβ/δ Antagonist, GSK3787, 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl)sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I
• 実験式（ヒル表記法）: C₁₅H₁₂ClF₃N₂O₃S
• CAS番号: 188591-46-0
• 分子量: 392.78
• MDL番号: MFCD00099612
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥99% (HPLC)
• フォーム: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: DMSO: 50 mg/mL, clear, colorless
• 輸送温度: ambient
• 保管温度: 2-8°C
• SMILES記法: FC(F)(F)c1cnc(cc1)[S](=O)(=O)CCNC(=O)c2ccc(cc2)Cl
• 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)
• InChI Key: JFUIMTGOQCQTPF-UHFFFAOYSA-N

詳細

詳細

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).

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

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

その他情報

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

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable