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化學性質:
規格 | 5mg 10mg 50mg 100mg |
CAS | 880635-03-0 |
別名 | N/A |
化學名 | (S,Z)-N-(3-(4-(2-(5-methyl-2-phenyloxazol-4-yl)ethoxy)phenyl)-2-((4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-en-2-yl)amino)propyl)propionamide |
分子式 | C35H36F3N3O4 |
分子量 | 619.67 |
溶解度 | DMF: 20 mg/ml,DMF:PBS(pH7.2) (1:2): 0.33 mg/ml,DMSO: 11 mg/ml,Ethanol: 10 mg/ml |
儲存條件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述:
GW 6471 is a potent PPARα antagonist.
In a cell-based reporter assay, GW 6471 completely inhibits GW409544-induced activation of PPARα with an IC50 of 0.24 μM[1]. 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, GW 6471 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, GW 6471 significantly and dose-dependently inhibits cell viability (up to approximately 80%) in both cell lines[2].
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, GW 6471 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 GW 6471-treated animals. No toxicity is observed at the doses of GW 6471 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 GW 6471, c-Myc levels are evaluated in the tumors, which show significant decreases in the GW 6471-treated animals[3].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278