| 名称 | GW9662 |
| 描述 | GW9662 (TIMTEC-BB SBB006523) is a PPARγ antagonist (IC50=3.3 nM) with selectivity. GW9662 can be used to study the pathogenesis of metabolic diseases, such as obesity and diabetes, by inhibiting the activity of PPARγ. GW9662 can be used to study the pathogenesis of inflammatory diseases, such as atherosclerosis and rheumatoid arthritis. GW9662 has anti-tumor effect. |
| 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) |
| 激酶实验 | Binding assay: The human PPARα, PPARγ, and PPARδ ligand binding domains (LBDs) are expressed in E. coli as polyhistidine-tagged fusion proteins. Receptors are immobilized on SPA beads by addition of the desired receptor (15 nM) to a slurry of streptavidin-modifed SPA beads (0.5 mg/mL) in assay buffer. The mixture is allowed to equilibrate for at least 1 hour at room temperature, and the beads are pelleted by centrifugation at 1×103 g. The supernate is discarded, and the beads are resuspended in the original volume of fresh assay buffer with gentle mixing. The centrifugation/resuspension procedure is repeated, and the resulting slurry of receptor-coated beads is used immediately or stored at 4 ℃ for up to 1 week before use. [3H]GW2443 are used as radioligands for determination of competition binding to PPARα, PPARγ, and PPARδ, respectively. Unless otherwise indicated, the buffer used for all assays is 50 mM HEPES (pH 7), 50 mM NaCl, 5 mM CHAPS, 0.1 mg/mL BSA, and 10 mM DTT. For some experiments, the HEPES (pH 7) is replaced with 50 mM Tris (pH 8). |
| 体外活性 | 方法：人乳腺癌肿瘤细胞系 （MCF7、 MDA-MB-468,、MDA-MB-231）用GW9662（(100 nM-50 mM）处理72小时，使用MTT实验检测细胞生长抑制情况。
结果：GW9662抑制MCF7、 MDA-MB-468,、MDA-MB-231细胞生长 （IC50=20 -30 μM）。[1] |
| 体内活性 | 方法：为研究GW9662对脂多糖保护作用的阻断作用，首先大鼠经脂多糖（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，再将GW9662（1 mg/kg）腹腔注射给大鼠。
结果：GW9662可阻断脂多糖的保护作用。[2] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 255 mg/mL (921.64 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (18.07 mM), Sonication is recommended.
Ethanol : 6.9 mg/mL (24.94 mM), Heating is recommended.
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| 关键字 | TIMTEC-BB SBB-006523 | TIMTEC-BB SBB 006523 | PPARδ | PPARγ | PPARα | PPAR | Peroxisome proliferator-activated receptors | Inhibitor | inhibit | GW-9662 | GW9662 |
| 相关产品 | Icariin | Daidzein | PHYTOL | Rosiglitazone | 5-Aminosalicylic Acid | Fenofibrate | Retinoic acid | 2,3-Butanediol | Cloxiquine | NPC 15199 | Naringenin | Maltitol |
| 相关库 | 抑制剂库 | 经典已知活性库 | 已知活性化合物库 | 抗胰腺癌化合物库 | 抗糖尿病库 | 抗衰老化合物库 | NO PAINS 化合物库 | 抗高血压化合物库 | 核受体化合物库 | 抗肥胖化合物库 | 神经退行性疾病化合物库 | 表型筛选靶点鉴定库 |