GSK0660

产品描述

GSK0660是一种选择性PPARβ拮抗剂，IC₅₀为0.155 µM。GSK0660对PPARα和PPARγ几乎无活性，IC₅₀大于10µM。GSK0660是PPARβ的配体，在细胞中能与激动剂竞争结合PPARβ，单独使用具有反向激动剂活性。GSK0660减少骨骼肌细胞中CPT1A和ANGPTL4的基础表达，但对PDK4的表达量没有影响 ^[1]。GSK0660以剂量依赖的方式降低血清诱导的人视网膜微血管内皮细胞的增殖和血管形成。玻璃体注射和腹膜注射GSK0660都能显著降低视网膜血管形成 ^[2]。GSK0660可以消除PPAR-δ 激动剂GW501516的效果，并能完全拮抗4-hydroxy-2E-nonenal对胰岛素分泌的放大作用 ^[3]。

靶点

GSK0660化学特性

GSK0660储存液配制

参考文献

[1] Shearer BG, et al. Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist. Mol Endocrinol. 22(2):523-9 (2008).

[2] Capozzi ME, et al. Peroxisome Proliferator-Activated Receptor-β/δ Regulates Angiogenic Cell Behaviors and Oxygen-Induced Retinopathy. Investigative Ophthalmology & Visual Science.54 (6):4197-4207(2013).

[3] Cohen G, et al. Role of Lipid Peroxidation and PPAR-δ in Amplifying Glucose-Stimulated Insulin Secretion. Diabetes 2011;60(11):2830-2842(2011).

[1] Lee G, et al. T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities. J Biol Chem. 277(22):19649-57(2002).

[2] Zaytseva YY, et al. The PPARgamma antagonist T0070907 suppresses breast cancer cell proliferation and motility via both PPARgamma-dependent and -independent mechanisms. Anticancer Res. Mar;31(3):813-23(2011).

[3] Collin M, et al. Peroxisome proliferator-activated receptor-gamma antagonists GW9662 and T0070907 reduce the protective effects of lipopolysaccharide preconditioning against organ failure caused by endotoxemia. Crit Care Med. 34(4):1131-8(2006).

GSK0660
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