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merck millipore,默克密理博,516567,PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem
产品名称:PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem
产品型号:516567
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.
merck millipore,默克密理博,516567,PPARβ/δ Antagonist, GSK3787 - CAS 188591-46-0 - Calbiochem
- 产品介绍
重要规格表
经验配方 CAS号 C₁₅H₁₂ClF₃N₂O₃S 188591-46-0 描述 概述 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). 产品目录编号 516567 品牌系列 Calbiochem®
同义词 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl) sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I 参考 参考 Palkar, P.S., et al. 2010. Mol. Pharmacol. 78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem. 53, 1857.产品信息 CAS号 188591-46-0 形式 White solid Hill配方 C₁₅H₁₂ClF₃N₂O₃S 化学配方 C₁₅H₁₂ClF₃N₂O₃S Molar Mass 392.8 结构配方图像 生物信息 纯度 ≥99% by HPLC 理化信息 溶解度 DMSO 储存和货运信息 货运代码 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
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