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生物活性
GW9662 acts as a potent, irreversible and selective PPARγ antagonist in both cell-free and cell-based assays. It modifies a cysteine residue in the ligand-binding site of PPARγ. In three breast cell lines including MCF7, MDA-MB-231 and MDA-MB-468, GW9662 suppresses the cell viability with IC50 values ranging from 20-30μM. In addition, GW9662 is reported to abolish the protection of LPS in a model of renal ischemia/reperfusion (I/R). In this model, the renal/glomerular dysfunction, tubular dysfunction and reperfusion injury caused by I/R can be significantly attenuated by LPS, and administration of GW9662 reverses this.
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体外研究
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体内研究
1% DMSO+30% polyethylene glycol+1% Tween 80
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激酶实验
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细胞实验
10 μM
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动物实验
1 mg/kg 腹腔注射
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不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Leesnitzer LM, et al. Biochemistry, 2002, 41(21), 6640-6650.
[2] Seargent, J.M., et al. 2004. Br. J. Pharmacol. 143: 933-937.
[3] Davies, G.F., et al. 2009. Drug Des Devel Ther. 3: 79-88.
[4] Huang, J.T., et al. 1999. Nature. 400: 378-382.
分子式
C13H9ClN2O3 |
分子量
276.68 |
CAS号
22978-25-2 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
26 mg/mL |
Water
Insoluble |
Ethanol
10 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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