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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
880635-03-0
- 规格：
10 mM * 1 mL/100 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1943.0 |
|---|---|---|---|
| 规格： | 100 mg | 产品价格： | 询价 |
| 规格： | 5 mg | 产品价格： | ￥1420.0 |
| 规格： | 10 mg | 产品价格： | ￥2280.0 |
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GW6471
CAS No. : 880635-03-0
MCE 国际站：GW6471
产品活性：GW6471 是一种有效的 PPARα 拮抗剂。
研究领域：Cell Cycle/DNA Damage | Vitamin D Related/Nuclear Receptor
作用靶点：PPAR
In Vitro: In a cell-based reporter assay, GW6471 completely inhibits GW409544-induced activation of PPARα with an IC50 of 0.24 μM. The functional role of PPARα is evaluated on renal cell carcinoma (RCC) cell viability by MTT assay. Both Caki-1 (VHL wild type) and 786-O (VHL mutated) cells are incubated separately with a specific PPARα agonist, WY14,643, or a specific PPARα antagonist, GW6471 at concentrations from 12.5 to 100 μM for 72 hours, and cell viability is assessed. While WY14,643 either has no affect on, or slightly increased, cell viability, GW6471 significantly and dose-dependently inhibits cell viability (up to approximately 80%) in both cell lines.
In Vivo: To test the antitumor activity of PPARα antagonism in vivo, a subcutaneous xenograft mouse model is used. Caki-1 cells are implanted subcutaneously in nude (Nu/Nu) mice. After tumor masses reach ～5 mm in diameter, GW6471 is administrated intraperitoneally every other day for 4 wk at a dose (20 mg/kg mouse body wt) that is described to be effective in an in vivo dose-response study and confirmed here to be efficacious. There are significant differences in tumor growth between vehicle- and GW6471-treated animals. No toxicity is observed at the doses of GW6471 based on weights of the animals, and laboratory values, including kidney and liver function tests, are not adversely affected. To demonstrate on-target effects of GW6471, c-Myc levels are evaluated in the tumors, which show significant decreases in the GW6471-treated animals.
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文献和实验magichunter 我在文献中查到，PPARr拮抗剂GW9662可以抑制药物的抗炎作用，前提是药物是通过激活PPARr来实现其抗炎作用的。即炎症细胞中的炎症因子（如：NO）升高，加入抗炎药物后，NO水平降低，当同时给予GW9662和该抗炎药物时，该药物的抗炎作用被抑制，NO水平再次升高。以上是文献的报道，但是我在实验时发现，加入了抗炎药物+GW9662后，NO的水平不但没有升高，反而降低了（与单独抗炎药物组相比），不知这是怎么回事？ chp
. A new drug candidate belonging to the family of the peroxisome proliferator-activated receptor-delta agonists termed GW1516 (also referred to as GW501516) has been prohibited by the World Anti-Doping Agency in 2009
有一种胖，反而有利于心血管健康！「肥胖悖论」新证据，源于脂肪
-HFD 喂养的 adipo-FtMT 小鼠心脏组织的蛋白质羰基化水平显著升高，且线粒体 H2O2 产生水平较对照小鼠显著增加。研究者根据这些数据提出大胆假设，即体内存在一种内分泌机制将促氧化信号从脂肪细胞传递到心肌。接下来，研究者通过纳米粒子追踪分析测量，发现食用 dox-HFD 3 周的 Adipo-FtMT 小鼠的循环 sEV 水平显著升高。进一步，利用中性鞘磷脂酶抑制剂 GW4869 阻断外泌体的产生，实验结果表明 dox-HFD 喂食 4 小时后，GW4869 完全阻止了 adipo
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