GW1929 is a synthetic peroxisome proliferator-activated receptor-γ (PPARγ) agonist with IC50 of 6.2 nM and 13 nM for human and mouse PPARγ, respectively.
GW1929 细胞实验
Cell Line
Concentration
Treated Time
Description
References
K562 cells
40 µM
1 hour
Overexpression of wild-type PPARγ in K562 cells significantly decreased OCT-1 activity (from 24.0 to 16.0 ng/200,000 cells, P=0.0286).
Haematologica. 2017 May;102(5):843-853.
HL60-BCRABL cells
40 µM
1 hour
GW1929 significantly decreased OCT-1 activity in HL60-BCRABL cells (from 11.9 to 8.9 ng/200,000 cells, P=0.0228), thereby reducing imatinib intracellular uptake and retention.
Haematologica. 2017 May;102(5):843-853.
KU812 cells
40 µM
1 hour
GW1929 significantly decreased OCT-1 activity in KU812 cells (from 10.8 to 7.5 ng/200,000 cells, P=0.0280), thereby reducing imatinib intracellular uptake and retention.
Haematologica. 2017 May;102(5):843-853.
OA chondrocytes
1 μM
GW1929, as a PPAR-γ agonist, was used to investigate its effects on the expression of inflammation and degeneration-related genes in OA chondrocytes. Results showed that GW1929 treatment significantly reduced the expression of TGF-β1, MMP-13, ADAMTS-4, ADAMTS-5, HtrA1, and iNOS, while increasing the expression of Collagen II.
J Orthop Translat. 2021 May 18;29:30-41.
Rat distal pulmonary arterial smooth muscle cells (PASMCs)
10 μM
48 h
GW1929 inhibited hypoxia-induced SOCE and caveolin-1 protein expression by 62.5% and 59.8% respectively through PPARγ activation.
A Caveolin-1-Dependent Mechanism. Am J Respir Cell Mol Biol.
macrophages
5 nM
6 h
GW1929 inhibited M1 polarization of macrophages under acidic conditions by decreasing the expression of iNOS and MCP-1, while increasing the expression of Arg-1 and CD206.
Front Immunol. 2021 Jun 21;12:697362.
J774 murine macrophages
10, 30, 100 µM
24 h
GW1929 inhibited LPS-induced iNOS expression and NO production in a dose-dependent manner
Arthritis Res Ther. 2013 Apr 17;15(2):R51.
pulmonary arterial smooth muscle cells (PASMCs)
10 µM
60 h
GW1929 significantly decreased TRPC1 and TRPC6 expression in PASMCs.
Am J Respir Cell Mol Biol. 2013 Aug;49(2):231-40.
GW1929 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Diabetic mice hindlimb ischemia model
Gavage
5 mg/kg
Twice daily for two weeks
To evaluate the role of PPAR γ on ischemia-induced angiogenesis. Results showed that GW1929 did not restore blood flow recovery and capillary density in diabetic mice.
Cardiovasc Diabetol. 2009 Sep 8;8:49
Guinea-pigs
Homologous β2-adrenoceptor desensitization model
Oral
1 mg/kg
Once daily for 6 days
GW1929 completely reversed salbutamol-induced β2-adrenoceptor tolerance in tracheal smooth muscle tissues derived from desensitized guinea-pigs, without changing salbutamol responsiveness in control animals.
Br J Pharmacol. 2011 Jan;162(2):378-91
Rats
Spontaneously hypertensive rats (SHR) and WKY rats
Oral
0.5 mg/kg
Once daily for 2 months
GW1929 significantly reduced systolic blood pressure (20±1%) and increased renal perfusion (61±3%) in SHR compared to WKY rats. Additionally, GW1929 improved renal vascular reactivity in SHR, including enhanced acetylcholine- and sodium nitroprusside-induced vasodilation and reduced phenylephrine-induced vasoconstriction. GW1929 also increased PPARγ mRNA expression (34±1%) while decreasing GRK-2 mRNA expression (31±3%).
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