Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 216 | 现货 | ||
5 mg | ¥ 492 | 现货 | ||
10 mg | ¥ 747 | 现货 | ||
25 mg | ¥ 1,160 | 现货 | ||
50 mg | ¥ 1,490 | 现货 | ||
100 mg | ¥ 1,930 | 现货 | ||
500 mg | ¥ 4,670 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 543 | 现货 |
产品描述 | 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. |
靶点活性 | PPARγ:3.3 nM |
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. |
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。 |
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). |
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) |
别名 | 2-氯-5-硝基-N-苯基苯酰胺, TIMTEC-BB SBB006523, GW 9662 |
分子量 | 276.68 |
分子式 | C13H9ClN2O3 |
CAS No. | 22978-25-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27.7 mg/mL (100 mM)
Ethanol: 6.9 mg/mL (25 mM)), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 3.6143 mL | 18.0714 mL | 36.1428 mL | 90.3571 mL |
5 mM | 0.7229 mL | 3.6143 mL | 7.2286 mL | 18.0714 mL | |
10 mM | 0.3614 mL | 1.8071 mL | 3.6143 mL | 9.0357 mL | |
20 mM | 0.1807 mL | 0.9036 mL | 1.8071 mL | 4.5179 mL | |
DMSO | 50 mM | 0.0723 mL | 0.3614 mL | 0.7229 mL | 1.8071 mL |
100 mM | 0.0361 mL | 0.1807 mL | 0.3614 mL | 0.9036 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
GW9662 22978-25-2 DNA Damage/DNA Repair Metabolism PPAR Peroxisome proliferator-activated receptors TIMTEC-BB SBB 006523 2-氯-5-硝基-N-苯基苯酰胺 TIMTEC-BB SBB-006523 Inhibitor inhibit TIMTEC-BB SBB006523 GW-9662 GW 9662 inhibitor