Potent, selective non-thiazolidinedione PPARγ partial agonist (EC50 = 57nM); produces ~25% maximum efficacy. Antagonizes full agonist activity by ~60% (IC50 ~ 285nM). Displays no activity at PPARα or PPARδ receptors. Produces altered receptor conformation, and regulates adipocyte development and gene expression, in a differential manner to full PPARγ agonists. Modulates metabolism and insulin sensitivity without causing cardiac hypertrophy in mice in vivo.
Chemical Name: 5-Chloro-1-[(4-chlorophenyl)methyl]-3-(phenylthio)-1H-indole-2-carboxylic acid
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