| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
GW1929 targets peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear receptor that regulates glucose and lipid metabolism, adipogenesis, and inflammation. PPARγ is the molecular target of thiazolidinedione (TZD) class of antidiabetic drugs. GW1929 is a highly selective PPARγ agonist with a pKi of 8.84 for human PPARγ. It shows negligible activity at PPARα and PPARδ (pEC₅₀ <4). Activation of PPARγ by GW1929 modulates gene expression involved in insulin sensitivity and inflammation.
|
|---|---|
| ln Vitro |
GW1929 Hydrochloride is a strong activator of PPAR-γ. Human PPAR-γ, PPAR-α, and PPAR-δ have respective pKs of 8.84, < 5.5, and < 6.5. The mouse PPAR and human PPAR-γ have pEC50 values of 8.56 and 8.56, respectively. 8.27 -γ, in that order [1]. In neocortical cell cultures, GW1929 hydrochloride (10 μM) suppresses TBBPA-induced caspase-3 activation and TBBPA-stimulated LDH release [2]. The levels of GW1929 hydrochloride considerably lower those of COX-2, iNOS, MMP-9, TNFα, and IL-6 [3].
GW1929 HCl is a potent PPARγ agonist with pEC₅₀ values of 8.56 for human PPARγ and 8.27 for murine PPARγ. It shows high selectivity over PPARα and PPARδ (pEC₅₀ <4). The compound exhibits antidiabetic activity by improving insulin sensitivity, as well as neuroprotective and anti-inflammatory effects. Specific IC₅₀ values for cellular activities are not extensively documented but are consistent with its potent PPARγ agonism. |
| ln Vivo |
After 14 days of treatment, Zucker diabetic obese (ZDF) rats treated with GW1929 hydrochloride (0.5, 1, 5 mg/kg) had significantly lower non-fasting blood glucose levels and showed anti-lipolytic effects [1]. In ZDF rats, GW1929 hydrochloride (1, 5 mg/kg) increases the amount of insulin secreted by β-cells in response to glucose [1]. In tumor-bearing mice, GW1929 hydrochloride (10 mg/kg body weight) reduces muscle loss during experimental cachexia [4].
GW1929 HCl has demonstrated antidiabetic efficacy in vivo, as well as neuroprotective and anti-inflammatory effects. The compound is orally active, making it suitable for in vivo studies. Specific in vivo efficacy data in animal models of diabetes, neurodegeneration, and inflammation are documented in the literature. Dosing and administration details are available from published studies. |
| Enzyme Assay |
The non-cellular receptor binding assay for GW1929 HCl typically involves measuring PPARγ binding affinity using a radioligand binding assay or a fluorescence polarization-based assay. PPARγ ligand-binding domain (LBD) is incubated with a fluorescent or radiolabeled PPARγ ligand and varying concentrations of GW1929 HCl. Displacement of the tracer ligand is measured, and IC₅₀ values are calculated. pKi values are determined from competition binding curves.
|
| Cell Assay |
In vitro cellular assays for GW1929 HCl typically use cell lines expressing PPARγ, such as 3T3-L1 adipocytes or reporter gene assays. In reporter gene assays, cells are transfected with a PPARγ-responsive luciferase reporter construct and treated with various concentrations of GW1929 HCl. Luciferase activity is measured to assess PPARγ activation. In adipocyte differentiation assays, 3T3-L1 preadipocytes are treated with GW1929 HCl and differentiation is assessed by Oil Red O staining and marker gene expression.
|
| Animal Protocol |
In vivo animal studies for GW1929 HCl typically involve rodent models of diabetes, obesity, or metabolic syndrome to evaluate its antidiabetic effects. GW1929 HCl is administered orally. Blood glucose, insulin levels, and lipid profiles are measured. Glucose tolerance tests and insulin sensitivity tests are performed. For neuroprotection studies, models of neurodegeneration are used, and behavioral and histological assessments are conducted. For anti-inflammatory studies, models of inflammation are employed.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of GW1929 HCl are characterized by its oral activity. The compound is soluble in water (53.2 mg/mL), facilitating oral administration. As a small molecule with molecular weight 532.03, it is expected to have reasonable oral bioavailability. Specific PK parameters such as half-life, Cmax, and protein binding are not extensively documented in the available literature.
|
| Toxicity/Toxicokinetics |
Toxicological data for GW1929 HCl are limited in the available literature. As a research-grade compound, comprehensive toxicology studies are not extensively documented. PPARγ agonists are generally well-tolerated, with common adverse effects including weight gain, fluid retention, and edema. However, specific toxicity data for GW1929 HCl are not available. Standard laboratory safety precautions should be observed when handling this compound.
|
| References |
|
| Additional Infomation |
GW1929 HCl is a research-grade compound intended for laboratory use only. It is not approved for clinical use as a therapeutic agent. Its primary applications include studying PPARγ biology and signaling, investigating the therapeutic potential of PPARγ agonists in diabetes, metabolic disorders, and neuroprotection, and serving as a reference compound in PPARγ-related research. The compound is also known as GW 1929 Hydrochloride.
|
| Molecular Formula |
C30H30CLN3O4
|
|---|---|
| Molecular Weight |
532.029906749725
|
| Exact Mass |
531.192
|
| CAS # |
1217466-21-1
|
| PubChem CID |
56972174
|
| Appearance |
Typically exists as solid at room temperature
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
12
|
| Heavy Atom Count |
38
|
| Complexity |
705
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
Cl.O(CCN(C)C1C=CC=CN=1)C1C=CC(=CC=1)C[C@@H](C(=O)O)NC1=CC=CC=C1C(C1C=CC=CC=1)=O
|
| InChi Key |
KXNKIKXTGRMLEY-YCBFMBTMSA-N
|
| InChi Code |
InChI=1S/C30H29N3O4.ClH/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);1H/t27-;/m0./s1
|
| Chemical Name |
(2S)-2-(2-benzoylanilino)-3-[4-[2-[methyl(pyridin-2-yl)amino]ethoxy]phenyl]propanoic acid;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8796 mL | 9.3980 mL | 18.7959 mL | |
| 5 mM | 0.3759 mL | 1.8796 mL | 3.7592 mL | |
| 10 mM | 0.1880 mL | 0.9398 mL | 1.8796 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
