| Bioactivity | GW1929 hydrochloride is an orally active peroxisome proliferator-activated receptor-γ (PPARγ) agonist with a pKi of 8.84 for human PPAR-γ, and pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, respectively. GW1929 hydrochloride has antidiabetic efficacy and neuroprotective potential. GW1929 hydrochloride suppresses neuronal apoptosis and shows anti-inflammatory potential[1][2][3]. |
| Invitro | GW1929 hydrochloride is a potent PPAR-γ activator, with pKis 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 hydrochloride (10 μM) inhibits TBBPA-induced caspase-3 increase and TBBPA-stimulated LDH release in neocortical cell cultures[2].GW1929 hydrochloride shows significant reduction in the COX-2, iNOS, MMP-9, TNFα and IL-6 levels[3]. |
| In Vivo | GW1929 hydrochloride (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[1].GW1929 hydrochloride (1, 5 mg/kg, p.o.) increases glucose-stimulated insuline secretion of β-cell in ZDF rats[1].GW1929 hydrochloride (10 mg/kg body weight) results in amelioration of muscle loss in tumour-bearing mice experimental cachexia[4]. |
| Name | GW1929 hydrochloride |
| CAS | 1217466-21-1 |
| Formula | C30H30ClN3O4 |
| Molar Mass | 532.03 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Brown KK, et al. A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat. Diabetes. 1999 Jul;48(7):1415-24. [2]. Wojtowicz AK, et al. PPAR-γ agonist GW1929 but not antagonist GW9662 reduces TBBPA-induced neurotoxicity in primary neocortical cells. Neurotox Res. 2014 Apr;25(3):311-22. [3]. Kaundal RK, et al. Ameliorative effects of GW1929, a nonthiazolidinedione PPARγ agonist, on inflammation and apoptosis in focal cerebral ischemic-reperfusion injury. Curr Neurovasc Res. 2011 Aug 1;8(3):236-45. [4]. Moore-Carrasco R, et al. Effects of the PPARgamma agonist GW1929 on muscle wasting in tumour-bearing mice. Oncol Rep. 2008 Jan;19(1):253-6. |