| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GSK376501A targets peroxisome proliferator-activated receptor gamma (PPARγ), a nuclear receptor that plays a crucial role in the regulation of glucose and lipid metabolism. It acts as a selective PPARγ modulator. PPARγ is a key regulator of adipocyte differentiation, insulin sensitivity, and inflammation. By modulating PPARγ activity, GSK376501A improves glycemic control and lipid metabolism in patients with type 2 diabetes.
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| ln Vitro |
In vitro, GSK376501A is a selective and effective modulator of PPARγ. As a PPARγ modulator, it regulates the expression of PPARγ target genes involved in glucose and lipid metabolism. Specific EC50 values for PPARγ activation are not detailed in the available sources. The compound's activity has been characterized in cell-based transactivation assays using PPARγ-responsive reporter genes.
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| ln Vivo |
GSK376501A has been developed for the treatment of type 2 diabetes mellitus. As a selective PPARγ modulator, it is expected to improve insulin sensitivity and glycemic control in vivo. The compound is designed to provide the beneficial effects of PPARγ activation while minimizing the side effects associated with full PPARγ agonists. Specific animal model data are not detailed in the available sources.
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| Enzyme Assay |
The PPARγ transactivation assay for GSK376501A involves using a GAL4-PPARγ fusion protein and a luciferase reporter gene containing GAL4 response elements. HEK293 cells are transfected with the GAL4-PPARγ expression plasmid and the reporter plasmid. Cells are treated with varying concentrations of GSK376501A for 24 hours, and luciferase activity is measured using a luminometer. EC50 values are calculated from dose-response curves.
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| Cell Assay |
To evaluate the cellular activity of GSK376501A, PPARγ-expressing cell lines (such as 3T3-L1 preadipocytes) are seeded in culture plates and treated with varying concentrations of GSK376501A. PPARγ target gene expression (such as adiponectin, aP2, and GLUT4) is measured by quantitative RT-PCR. Adipocyte differentiation can be assessed by Oil Red O staining. The EC50 for induction of target gene expression or adipocyte differentiation is calculated.
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| Animal Protocol |
The in vivo efficacy of GSK376501A is evaluated in animal models of type 2 diabetes, such as db/db mice or high-fat diet-induced obese mice. Rodents are treated with GSK376501A orally at various doses for a specified period. Blood glucose, insulin, and lipid levels are measured. Glucose tolerance tests and insulin tolerance tests are performed to assess improvements in glycemic control. The compound's effects on body weight and adipose tissue are also monitored.
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| ADME/Pharmacokinetics |
GSK376501A is soluble in DMSO at 100 mg/mL (188.10 mM). Specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available sources. The compound has a molecular weight of 531.64 and a molecular formula of C32H37NO6. As a powder, it is stable at -20°C for 3 years and at 4°C for 2 years. In solvent, it can be stored at -80°C for 6 months.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GSK376501A are not provided in the available sources. As a research compound, it is intended for laboratory use only and is not approved for human therapeutic applications. The compound is a selective PPARγ modulator, and its safety profile would be expected to be consistent with other PPARγ modulators. Standard safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
GSK376501 has been used in trials investigating the treatment and diagnosis of type 2 diabetes.
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus. It has a molecular formula of C32H37NO6 and a molecular weight of 531.64. It is a small molecule drug developed by GlaxoSmithKline. The compound is supplied for research purposes with a purity of >98%. |
| Molecular Formula |
C32H37NO6
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|---|---|
| Molecular Weight |
531.6393
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| Exact Mass |
531.262
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| CAS # |
1010412-80-2
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| PubChem CID |
24946920
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| Appearance |
White to off-white solid powder
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| LogP |
6.402
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
39
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| Complexity |
729
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OIDYMQICWGYEDR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H37NO6/c1-32(2,3)24-12-10-23(11-13-24)29-27-8-6-7-9-28(27)33(30(29)31(34)35)21-22-18-25(38-16-14-36-4)20-26(19-22)39-17-15-37-5/h6-13,18-20H,14-17,21H2,1-5H3,(H,34,35)
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| Chemical Name |
1-[[3,5-bis(2-methoxyethoxy)phenyl]methyl]-3-(4-tert-butylphenyl)indole-2-carboxylic acid
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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 : ~100 mg/mL (~188.10 mM)
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| 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 | 1.8810 mL | 9.4049 mL | 18.8097 mL | |
| 5 mM | 0.3762 mL | 1.8810 mL | 3.7619 mL | |
| 10 mM | 0.1881 mL | 0.9405 mL | 1.8810 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.
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