| 货号 | 15219-50mg |
| 描述 | PPARβ/δ is thought to play a role in lipid homeostasis and glucose disposal by regulating genes involved in fatty acid oxidation, reverse cholesterol transport, and carbon substrate utilization in skeletal muscle. It has also been implicated in the progression of certain cancers.1,2,3,4 GSK3787 is an irreversible antagonist of PPARβ/δ (pIC50 = 6.6) with no measurable affinity for PPARα or PPARγ (pIC50>5).5 At 1μM, it inhibits the expression of PPARβ/δ-regulated target genes, pyruvate dehydrogenase kinase 4 and carnitine palmitoyl transferase 1a, which are important for energy homeostasis in human skeletal muscle cells.5 GSK3787 (at 1 μM) also antagonizes agonist-induced expression of angiopoietin-like protein 4 in mouse fibroblasts, mouse keratinocytes, and human MCF-7, Huh7, and HepG2 cancer cell lines.6 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Michalik, L.,Desvergne, B. and Wahli, W. Peroxisome-proliferator-activated receptors and cancers: Complex stories. Nature Reviews.Cancer 4, 61-70 (2004). 2.Girroir, E.E.,Hollingshead, H.E.,Billin, A.N., et al. Peroxisome proliferator-activated receptor-ß/δ (PPAR ß/δ) ligands inhibit growth of UACC903 and MCF7 human cancer cell lines. Toxicology 243, 236-243 (2008). 3.Peters, J.M.,Foreman, J.E. and Gonzalez, F.J. Dissecting the role of peroxisome proliferator-activated receptor-ß/δ (PPARß/δ) in colon, breast, and lung carcinogenesis. Cancer Metastasis Reviews 30, 619-640 (2011). 4.Elikkottil, J.,Kohli, D.R. and Gupta, K. Antitumor activity of a PPARδ antagonist. Cancer Biology and Therapy 8(13), 1262-1264 (2009). 5.Shearer, B.G.,Wiethe, R.W.,Ashe, A., et al. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist. Journal of Medicinal Chemistry 53, 1857-1861 (2010). 6.Palkar, P.S.,Borland, M.G.,Naruhn, S., et al. Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-β/δ antagonist GSK3787. Molecular Pharmacology 78(3), 419-430 (2010). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 392.8 |
| 分子式 | C15H12ClF3N2O3S |
| CAS号 | 188591-46-0 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |