Drug intelligence / Profile preview

GW6471

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral (research Context, E.g., Gavage In Mice), In Vitro (cell Culture Studies)
01

Overview

GW6471 is a **potent and selective antagonist of the peroxisome proliferator-activated receptor alpha (PPARα)**. It inhibits PPARα by enhancing the recruitment of co-repressors and displacing coactivators, with **an IC50 of approximately 0.24 μM**[3][5][9]. GW6471 has been widely used in research to study metabolic diseases and cancer by modulating fatty acid metabolism, glucose metabolism, and inflammation. In preclinical models, GW6471 has demonstrated the ability to: - **Reduce obesity, hepatic steatosis, and insulin resistance** in mouse models of non-alcoholic steatohepatitis (NASH) and high-fat diets by inhibiting intestinal PPARα activity[1]. - **Induce apoptosis and cell cycle arrest** in renal cell carcinoma (RCC) and breast cancer stem cells, and attenuate tumor growth in xenograft mouse models[2][4][6][5]. - **Block viral infections**, such as SARS-CoV-2 in airway organoids, by downregulating HIF1α and associated pathways[5]. - Modulate metabolic reprogramming in cancer cells by reducing fatty acid oxidation, glycolysis, and affecting c-Myc regulation[2][4]. GW6471 is **intended for laboratory research use only** and is not approved for clinical use.

Other names
GW 6471GW6471GW-6471
02

Targets

PPARA (Peroxisome proliferator-activated receptor alpha)

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