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Chemical Structure| 196808-24-9 Chemical Structure| 196808-24-9

Structure of GW1929
CAS No.: 196808-24-9

Chemical Structure| 196808-24-9

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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.

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Product Details of GW1929

CAS No. :196808-24-9
Formula : C30H29N3O4
M.W : 495.57
SMILES Code : O=C(O)[C@@H](NC1=CC=CC=C1C(C2=CC=CC=C2)=O)CC3=CC=C(OCCN(C)C4=NC=CC=C4)C=C3
MDL No. :MFCD04040003

Safety of GW1929

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Isoform Comparison

Biological Activity

In Vitro:

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.

In Vivo:

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%). Am J Nephrol. 2009;30(3):201-8

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.02mL

0.40mL

0.20mL

10.09mL

2.02mL

1.01mL

20.18mL

4.04mL

2.02mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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