| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
GW1929 is a novel, potent and selective PPAR-γ 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. With a 1.4 nM Ki value, GW-1929 exhibits more than 1,000-fold selectivity over other PPAR subtypes. The role of Egr-1 in PPARγ-independent activation of p38 MAPK and inactivation of PI3-K/mTOR is how GW1929 suppresses the expression of α7 nAChR. By lowering inflammation and DNA fragmentation, GW1929 lessens neurological damage in cases of global cerebral ischemia-reperfusion injury.
| Targets |
PPAR-γ (pEC50 = 8.56)
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| ln Vitro |
GW1929 is an effective PPAR-γ activator, having pKi values of 8.84, <5.5, and <6.5 for human, PPAR-α, and PPAR-δ, respectively, and pEC50 values for human and mouse PPAR-γ. When TBBPA is added to freshly activated cell cultures, it inhibits the rise of caspase-3 and the release of LDH, as demonstrated by GW1929 (10 μM). with 8.56 and 8.27[1].
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| ln Vivo |
After 14 days of treatment, GW1929 (0.5, 1, 5 mg/kg, flour) had anti-lipolytic effects, certain non-fasting chest glucose levels, and a significant reduction in Zucker diabetes mellitus (ZDF). In higher ZDF, GW1929 (1,5 mg/kg, po) increases β-cell death [1].
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| Enzyme Assay |
The scintillation proximity assay (SPA) is used to measure ligand binding to the bacterially expressed ligand binding domain (LBD) of hPPAR-γ. The test assesses potential ligands' capacity to displace receptor-bound [3H]BRL 49653. Assays are run in plates with 96 wells. The wells held different concentrations of either troglitazone or GW1929; streptavidin-modified SPA beads that were prebound with biotinylates PPAR-γ LBD; and 10 nM of the particular radioligand [3H]BRL 49653 in a 100 μL volume. Each data point has its amount of nonspecific binding subtracted, as determined by control wells containing 50 μM of the corresponding unlabeled ligand. With the assumption of simple competitive binding, apparent Ki values are estimated from a nonlinear least squares fit of the data for each compound tested. Plots of ligand concentration versus counts/min of radioligand bound are then created. In order to express the results, we use pKi, where pKi = -log10(Ki)[1].
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| Cell Assay |
In the experiments, the cells are cultured in the presence of TBBPA at concentrations ranging from 1 nM to 100 μM after being plated at a density of 2 × 105 cells per cm2 in 96-well plates. After dissolving TBBPA in DMSO, the vehicle concentration is reduced to 0.1% (v/v). The experimental design includes both vehicle-free control and DMSO-treated wells to ascertain the impact of DMSO. To investigate the potential role of PPAR-γ in the neurotoxic effects of TBBPA, cells are co-treated with 10 μM GW1929 or GW9662 along with 10 μM TBBPA. Following either six or twenty-four hours of culture, 100 microliters of medium are taken for the LDH analysis, and the cells are taken and frozen at -70°C to measure the activity of caspase-3[2].
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| Animal Protocol |
The animals live in housing with a 12-hour light and dark cycle, 50% relative humidity, and 72°F temperature. They are fed Formulab Diet 5008. Male Zucker diabetic fatty rats that are age- and glucose-matched are gavaged twice a day for 14 days with either vehicle (0.05 M N-methylglucamine), GW1929 (0.5, 1.0, or 5.0 mg/kg), or troglitazone (as the milled extrudate in a methylcellulose suspension, 50, 150, and 500 mg/kg). A combination of humulin N and humulin R is injected subcutaneously twice a day into another set of animals. Nonfasted measurements of glucose, lactate, insulin, total cholesterol, TGs, F FAs, and hematocrit are taken on days 7 and 14 of dosing. Samples for glycosylated hemoglobin measurements and serum drug levels are also taken on day 14 of dosing, two hours after the dose. Furthermore, three animals from each group are put in metabolic chambers for 48 hours once a week to measure how much food and water they consume in a 24-hour period. Body weight is tracked for the duration of the research. In order to directly assess the effects of treatment on basal and glucose-stimulated insulin secretion, perfused pancreas experiments are carried out on 12 animals (n = 4 per group) that have received either GW1929 (1 and 5 mg/kg) or vehicle at the end of the study.
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| 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 |
| Molecular Formula |
C30H29N3O4
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|---|---|
| Molecular Weight |
495.56896
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| Exact Mass |
495.22
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| Elemental Analysis |
C, 72.71; H, 5.90; N, 8.48; O, 12.91
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| CAS # |
196808-24-9
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| Related CAS # |
196808-24-9
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| Appearance |
Solid powder
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| SMILES |
CN(CCOC1=CC=C(C=C1)C[C@@H](C(=O)O)NC2=CC=CC=C2C(=O)C3=CC=CC=C3)C4=CC=CC=N4
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| InChi Key |
QTQMRBZOBKYXCG-MHZLTWQESA-N
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| InChi Code |
InChI=1S/C30H29N3O4/c1-33(28-13-7-8-18-31-28)19-20-37-24-16-14-22(15-17-24)21-27(30(35)36)32-26-12-6-5-11-25(26)29(34)23-9-3-2-4-10-23/h2-18,27,32H,19-21H2,1H3,(H,35,36)/t27-/m0/s1
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| Chemical Name |
(2S)-2-(2-benzoylanilino)-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]propanoic acid
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| Synonyms |
GW 1929; GW1929; GW-1929
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ≥ 35 mg/mL (~70.6 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0179 mL | 10.0894 mL | 20.1788 mL | |
| 5 mM | 0.4036 mL | 2.0179 mL | 4.0358 mL | |
| 10 mM | 0.2018 mL | 1.0089 mL | 2.0179 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Representative Western blot of PPAR-γ protein levels in neocortical neurons treated with TBBPA (10μM); GW1929 (10μM); cells co-treated with GW1929 (10μM) and TBBPA (10μM); GW9662 (10μM); cells co-treated with GW9662 (10μM) and TBBPA (10μM) (a). PPAR-γ bands were quantified by densitometry.Neurotox Res.2014 Apr;25(3):311-22. |
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 The effect of 10μM of TBBPA on the caspase-3aand LDHbactivity in the presence of PPAR-γ agonist GW1929 in neocortical neuron cultures after 6 and 24h of exposure.Neurotox Res.2014 Apr;25(3):311-22. |
 The effect of TBBPA on Hoechst 33342 staining in neocortical neuron cell cultures, examined 24h post treatment,acontrol cells;bTBBPA-treated cells (10μM);cGW1929-treated cells;dcells co-treated with GW1929 (10μM) and TBBPA (10μM);eGW9662-treated cells;fcells co-treated with GW9662 (10μM) and TBBPA (10μM).Neurotox Res.2014 Apr;25(3):311-22. |
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