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GW6471

CAS No. : 880635-03-0

MCE 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

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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