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GW1929

SKU: orb1296168

Description

GW1929 is a high-affinity and potent agonist of the peroxisome proliferator-activated receptor gamma (PPAR-γ), with demonstrated activity in both human and murine systems. This small molecule is a valuable research tool for studying PPAR-γ signaling in metabolic diseases, including diabetes and obesity, in various in vitro and in vivo models.

Research Area

Metabolism Research, Molecular Biology

Images & Validation

Key Properties

CAS Number196808-24-9
MW495.57
Purity98.21% (May vary between batches)
FormulaC30H29N3O4
SMILESCN(CCOc1ccc(C[C@H](Nc2ccccc2C(=O)c2ccccc2)C(O)=O)cc1)c1ccccn1
TargetPPAR
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.04 mM);DMSO:33 mg/mL (66.59 mM)

Bioactivity

Target IC50
PPARγ (human):8.84 (pKi)
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. In ZDF rats, GW1929 (1, 5 mg/kg, p.o.) increases glucose-stimulated insulin secretion of β-cell .
In Vitro
GW1929 is a potent PPAR-γ activator, with pEC50s of 8.56 and 8.27 for human PPAR-γ and murine PPAR-γ, and pKis of 8.84, < 5.5, and < 6.5 for human PPAR-γ, PPAR-α, and PPAR-δ, respectively . GW1929 (10 μM) inhibits TBBPA-induced caspase-3 increase and TBBPA-stimulated LDH release in neocortical cell cultures .
Cell Research
For the experiments, the cells are plated in 96-well plates at a density of 2 × 10^5 cells per cm2 and cultured in the presence of TBBPA, in concentrations ranging from 1 nM to 100 μM TBBPA. TBBPA is dissolved in DMSO, resulting in a final vehicle concentration of 0.1 % (v/v). Control (no vehicle) and DMSO-treated wells are included in the experimental design to determine the effect of DMSO. To study whether PPAR-γ is involved in the neurotoxic effect of TBBPA, cells are co-treated with 10 μM TBBPA and 10 μM GW1929 or GW9662. After 6 or 24 h of culture, 100 μL medium is collected for the LDH analysis, and the cells are collected and frozen at 70°C for the caspase-3 activity measurements .
Animal Research
Animals are housed at 72°F and 50% relative humidity with a 12-h light and dark cycle and fed Formulab Diet 5008. Age- (60-day) and glucose-matched male Zucker diabetic fatty rats are gavaged twice daily for 14 days with vehicle (0.05 M N-methylglucamine), GW1929 (0.5, 1.0, or 5.0 mg/kg), or troglitazone (as the milled extrudate, in a suspension in methylcellulose, 50, 150, and 500 mg/kg). Another group of animals receives a mixture of Humulin N and Humulin R by subcutaneous injection twice daily. On days 7 and 14 of dosing, nonfasted measurements of glucose, lactate, insulin, total cholesterol, TGs, F FAs, and hematocrit are obtained. On day 14 of dosing, samples for serum drug levels (2-h postdose) and glycosylated hemoglobin measurements are also collected. In addition, once weekly, three animals from each group are placed in metabolic chambers for 48 h for quantitation of 24-h food and water consumption. Body weights are recorded throughout the study. At the conclusion of the study, perfused pancreas experiments are performed on 12 animals (n = 4 per group) that have received either GW1929 (1 and 5 mg/kg) or vehicle, to directly evaluate the effects of treatment on basal and glucose-stimulated insulin secretion. The remaining animals are killed, and their pancreases are processed for immunocytochemistry .

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

GW1929, GW-1929, GW 1929, Inhibitor, inhibit, Peroxisome proliferator-activated receptors, PPAR, PPARγ

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  • GW1929 [orb1219714]

    >98% (HPLC)

    196808-24-9

    495.57

    C30H29N3O4

    1 g, 500 mg, 200 mg, 50 mg, 100 mg, 25 mg, 10 mg, 5 mg
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Key Properties

No computed properties available.

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GW1929 (orb1296168)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

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1 mg
$ 70.00
5 mg
$ 110.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 160.00
25 mg
$ 280.00
50 mg
$ 470.00
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