118414-59-8

nTZDpa is a PPARγ agonist, with pharmaceutical applications such as anti-diabetic drugs.

Potent, selective non-thiazolidinedione PPAR γ partial agonist (EC 50 = 57 nM); produces ~25% maximum efficacy. Antagonizes full agonist activity by ~60% (IC 50 ~ 285 nM). Displays no activity at PPAR α or PPAR δ receptors. Produces altered receptor conformation, and regulates adipocyte development and gene expression, in a differential manner to full PPAR γ agonists. Modulates metabolism and insulin sensitivity without causing cardiac hypertrophy in mice in vivo .

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