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化驗
>98% (HPLC)
形狀
powder
顏色
white
溶解度
DMSO: 26 mg/mL
H2O: insoluble
儲存溫度
2-8°C
SMILES 字串
[O-][N+](=O)c1ccc(Cl)c(c1)C(=O)Nc2ccccc2
InChI
1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17)
InChI 密鑰
DNTSIBUQMRRYIU-UHFFFAOYSA-N
基因資訊
human ... PPARG(5468)
應用
Gw9662用作过氧化物酶体增殖物激活受体 γ (PPARγ)的拮抗剂,存在于人类多能干细胞中 也存在于去氧肾上腺素刺激的心肌细胞中 并抑制替米沙坦嗜铬细胞瘤PC12细胞的保护作用。
生化/生理作用
GW9662是一种不可逆的PPARγ拮抗剂。GW9662可抑制结缔组织生长因子,并通过IL-4激活CD36。
GW9662是一种不可逆的PPARγ拮抗剂;可抑制结缔组织生长因子,并通过IL-4激活CD36。
Gw9662(2-氯-5-硝基苯甲酰苯胺)与过氧化物酶体增殖物激活受体 γ (PPARγ)的配体结合位点结合,抑制脂肪细胞分化。即使在PPARγ 激动剂罗格列酮存在的情况下,它也有利于抑制乳腺癌细胞系的细胞生长。它刺激M2c巨噬细胞分化,触发生长停滞特异性蛋白6(Gas6)的表达。GW9662与其他PPARγ 配体联合使用,可对胶质母细胞瘤干细胞产生抗增殖作用,可能会成为有效的治疗剂。
法律資訊
根据GlaxoSmithKline协议,仅为研究目的出售
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
其他客户在看
Bezafibrate attenuates pressure overload-induced cardiac hypertrophy and fibrosis
PPAR Research, 2017(43), 26303-26313 (2017)
Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662
Biochemistry, 41(21), 6640-6650 (2002)
The synergistic enhancement of cloning efficiency in individualized human pluripotent stem cells by peroxisome proliferative-activated receptor-gamma (PPARgamma) activation and rho-associated kinase (ROCK) inhibition
The Journal of Biological Chemistry, 290(43), 26303-26313 (2015)
GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation
British Journal of Pharmacology, 143(8), 933-937 (2004)
Molecular medicine (Cambridge, Mass.), 14(7-8), 403-411 (2008-05-14)
PPARgamma, a member of the peroxisome proliferator-activated receptor family, is overexpressed in prostate cancer. Natural and synthetic ligands of PPARgamma via genomic and nongenomic actions promote cell cycle arrest and apoptosis of several prostate cancer cells, in vitro. Insulin-like growth
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