GW1929

GW 1929 is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pK_i of 8.84 for human PPAR-γ, and pEC₅₀s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW 1929 (hydrochloride) has antidiabetic efficacy and neuroprotective potential^[1][2]. IC50 & Target: pKi: 8.84 (Human PPAR-γ), < 5.5 (Human PPAR-α), < 6.5 (Human PPAR-δ)^[1]
pEC50: 8.56 (Human PPAR-γ), 8.27 (Murine PPAR-γ)^[1] In Vitro: GW1929 is a potent PPAR-γ activator, with pK_is of 8.84, < 5.5, and < 6.5 for human PPAR-γ, PPAR-α, and PPAR-δ, and pEC₅₀s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively^[1]. GW1929 (10 μM) inhibits TBBPA-induced caspase-3 increase and TBBPA-stimulated LDH release in neocortical cell cultures^[2]. In Vivo: GW1929 (0.5, 1, 5 mg/kg, p.o.) highly decreases nonfasted plasma glucose levels in Zucker diabetic fatty (ZDF) rats after treatment for 14 days, and possesses antilipolytic efficacy. GW1929 (1, 5 mg/kg, p.o.) increases glucose-stimulated insuline secretion of β-cell in ZDF rats^[1].