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GW9662

GW9662 (TIMTEC-BB SBB006523) 是一种特异性 PPARγ 拮抗剂，IC50值为3.3 nM，在细胞中对 PPARγ 的功能选择性是 PPARα/δ 的 10 到 1000 倍。

CAS号

22978-25-2

分子式

C13H9ClN2O3

主要靶点

PPAR

仅限科研使用

Cat No : CM00289

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Synonyms

GW 9662|TIMTEC-BB SBB006523|2-氯-5-硝基-N-苯基苯酰胺

验证数据展示

  • CAS No.: 22978-25-2

    GW9662
    CAS#: 22978-25-2

产品信息

GW9662 (TIMTEC-BB SBB006523) is a specific PPARγ antagonist (IC50: 3.3 nM, in a cell-free assay), with 100 to 1000-fold functional selectivity for PPARγ than PPARα/δ in cells.

CAS号 22978-25-2
分子式 C13H9ClN2O3
主要靶点 PPAR
主要通路 DNA损伤和修复|代谢
分子量 276.68
纯度 99.94%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GW 9662|TIMTEC-BB SBB006523|2-氯-5-硝基-N-苯基苯酰胺

靶点活性

PPARγ:3.3 nM

体内活性

GW9662抑制PPARγ激活,并抑制人乳腺癌肿瘤细胞系（MCF7, MDA-MB-468, MDA-MB-231）生长（IC50：20 -30 μM）。GW9662结合PPARγ上的Cys(285),其是三种PPAR中较保守的。在MDA-MB-231细胞中,Rosiglitazone（50 μM）与GW9662（10 μM）联用7天后,其存活细胞数的减少程度具有统计学意义。在原代鼠骨髓和RAW264.7细胞中,PPARγ1配体对RANKL诱导的破骨细胞形成有抑制作用,而GW 9662（2 μM）可浓度依赖性地逆转这些配体的抑制作用。在RAW264.7细胞中,GW 9662（1 μM）抑制NF-κB的RANKL激活。 在BMs中,GW 9662（2 μM）阻断IL-4对破骨细胞形成的抑制。在甲状腺眼病患者的原代前脂肪细胞中,GW9662（10 μM）对激素和激动剂诱导的脂肪细胞分化有抑制作用。

体外活性

大鼠经脂多糖（1 mg/kg,i.p.）预处理,可明显减弱肾损伤和功能障碍引起的所有缺血/再灌注损伤特征.而GW9662（1 mg/kg,i.p.）可阻断脂多糖的保护作用.

溶解度

DMSO:27.7 mg/mL (100 mM),Ethanol:6.9 mg/mL (25 mM)),with gentle warming

细胞实验

MDA-MB-231 cells are seeded at a density of 1 × 105 cells per 25 cm3 tissue culture flask. After 24 h (day 0), the growth medium is replaced with fresh medium containing rosiglitazone (50 μM), GW9662 (10 μM) or both together. Control flasks receives 0.1% DMSO. Cells are harvested on days 0, 3, 5, 7, 10 for each treatment condition by trypsinisation, stained using trypan blue, and the total and viable number of cells per flask calculates using a haemocytometer.(Only for Reference)

参考文献

1.Leesnitzer LM, et al. Biochemistry, 2002, 41(21), 6640-6650.
2.Miao Y, Zhang Y, Qiao S, et al. Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon[J]. Acta Pharmacologica Sinica. 2020: 1-14.
3.Seargent JM, et al. Br J Pharmacol, 2004, 143(8), 933-937.
4.Bendixen AC, et al. Proc Natl Acad Sci U S A, 2001, 98(5), 2443-2448.
5.Starkey K, et al. J Clin Endocrinol Metab, 2003, 88(1), 55-59.
6.Collino M, et al. Kidney Int, 2005, 68(2), 529-536.
7.Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101(1):57-67.
8.Qiao N, Lin Y, Wang Z, et al. Maresin1 Promotes M2 Macrophage Polarization Through peroxisome proliferator–activated receptor-γ Activation to Expedite Resolution of Acute Lung Injury[J]. Journal of Surgical Research. 2020, 256: 584-594.
9.Lin X, Ma Y, Qian T, et al. Basic Fibroblast Growth Factor Promotes Prehierarchical Follicle Growth and Yolk Deposition in the Chicken[J]. Theriogenology. 2019.
10.Zong X, Wang H, Xiao X, et al. Cathelicidin-WA facilitated intestinal fatty acid absorption through enhancing PPAR-γ dependent barrier function[J]. Frontiers in immunology. 2019, 10: 1674.

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