<Suppliers Price>

GW 1929 hydrochloride

Names

[ CAS No. ]:
1217466-21-1

[ Name ]:
GW 1929 hydrochloride

[Synonym ]:
L-Tyrosine, N-(2-benzoylphenyl)-O-[2-(methyl-2-pyridinylamino)ethyl]-, hydrochloride (1:1)
MFCD28359221
N-(2-Benzoylphenyl)-O-{2-[methyl(2-pyridinyl)amino]ethyl}-L-tyrosine hydrochloride (1:1)

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> PPAR
Research Areas >> Inflammation/Immunology
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease

[Target]

hPPARγ:8.84 (pKi)


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H30ClN3O4

[ Molecular Weight ]:
532.030

[ Exact Mass ]:
531.192505

[ Appearance of Characters ]:
GW1929

[ Storage condition ]:
store at -20℃ for one year（Powder）

Related Compounds