hpparα

Muraglitazar (BMS-298585) is a PPAR α γ dual agonist for the treatment of type 2 diabetes and associated dyslipidemia. Muraglitazar shows potent activity in vitro at human PPARα and PPARγ with EC50 of 320 nM and 110 nM respectively.

NXT629 is a selective and highly efficient PPAR-α antagonist with anticancer activity. It inhibits PPARδ, PPARγ, Erβ, GR, and TRβ and can be used in research on ovarian cancer and melanoma.

GW 501516 (Endurobol) is a effective and highly specifc PPARβ δ agonist (EC50: 1 nM), with 1000-fold selectivity over hPPARα γ.

LT175, a dual PPARα γ ligand, demonstrates potent insulin-sensitizing effects with reduced adipogenic properties. This orally active partial agonist targets PPARγ with EC50 values of 0.22 μm for hPPARα, 0.26 μm for mPPARα, and 0.48 μm for hPPARγ. LT175 specifically interacts with PPARγ, influencing the recruitment of coregulators, such as the cyclic-AMP response element-binding protein-binding protein and nuclear corepressor 1 (NCoR1), within a hydrophobic region known as the diphenyl pocket [1].