GSK1292263
Based on 7 publication(s) in Google Scholar
GSK-1292263 is an orally available GPR119 agonist with pEC50s of 6.9 and 6.7 for human and rat GPR119, respectively. GSK-1292263 can be used for the research of type 2 diabetes mellitus (T2DM).
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- Pureté: 98.68%
- CAS No.: 1032823-75-8
- Formule: C23H28N4O4S
- Masse moléculaire:456.56
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) GSK1292263
More- Nat Chem. 2025 Apr 3. [Abstract]
- J Exp Clin Cancer Res. 2018 Nov 29;37(1):295. [Abstract]
- J Ethnopharmacol. 2026 Apr 30:121790. [Abstract]
- Biomol Ther (Seoul). 2026 May 1;34(3):666-675. [Abstract]
- FASEB J. 2016 Jan;30(1):324-35. [Abstract]
- bioRxiv. 2025 Oct 17.
- College of Pharmacy. Seoul National University. 2015 Aug.
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WB
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Activité biologique
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male neonatal Streptozotocin (STZ)-induced SD rats (7 weeks of age)[2]
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Dosage:30 mg/kg
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Administration:Orally given; once a day for 2 weeks
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Result:The AUC of plasma glucose (AUCPG) in the single treatment of the GSK1292263 group was numerically lower than that of the vehicle group, but the effect was modest.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1032823-75-8
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Appearance Solid
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Masse moléculaire 456.56
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Formule C23H28N4O4S
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Color White to off-white
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SMILES
CC(C1=NOC(N2CCC(CC2)COC3=CN=C(C=C3)C4=CC=C(C=C4)S(C)(=O)=O)=N1)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Chem
2025 Apr 3. PMID: 40181149 -
J Exp Clin Cancer Res
GPR119 agonist enhances gefitinib responsiveness through lactate-mediated inhibition of autophagy. [Abstract]2018 Nov 29;37(1):295. PMID: 30497501 -
J Ethnopharmacol
Tianwang Buxin Decoction ameliorates neuroinflammation in insomnia via adenosine accumulation-mediated AMPK/SIRT1 pathway. [Abstract]2026 Apr 30:121790. PMID: 42069163 -
Biomol Ther (Seoul)
2026 May 1;34(3):666-675. PMID: 42059036 -
FASEB J
2016 Jan;30(1):324-35. PMID: 26399788
GSK1292263 purchased from MedChemExpress. Usage Cited in: FASEB J. 2016 Jan;30(1):324-35. [Abstract]
Treatment with 2 synthetic GPR119 agonists, MBX-2982 (MBX) and GSK1292263 (GSK), suppresses T090-induced SREBP-1 expression and mRNA levels of SREBP-1 target genes such as FAS, ACC, and SCD-1.
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GSK1292263 purchased from MedChemExpress. Usage Cited in: College of Pharmacy. Seoul National University. 2015 Aug.
Effects of GPR119 ligands on T090-induced pSREBP-1 and lipogenic enzymes expression. Primary cultured hepatocytes from GPR119-WT and -KO mice and HepG2 cells are pretreated with two GPR119 ligands [(MBX (MBX-2982) or GSK (GSK1292263)] for 30 min and the cells are exposed to T090 for 12 h.
Solvant et solubilité
DMSO : ≥ 20 mg/mL (43.81 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (596 KB)
- English - EN (596 KB)
- Français - FR (596 KB)
- Deutsch - DE (596 KB)
- Norwegian - NO (596 KB)
- Español - ES (596 KB)
- Swedish - SV (596 KB)
- Italian - IT (596 KB)
- Korean - KR (596 KB)
- Portuguese - PT (596 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. X. Zhu, et al. GPR119 Agonists: A Novel Strategy for Type 2 Diabetes Treatment.
[2]. Koji Matsumoto, et al. DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats. J Pharmacol Exp Ther. 2018 Dec;367(3):509-517. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1903 mL | 10.9515 mL | 21.9029 mL | 54.7573 mL |
| 5 mM | 0.4381 mL | 2.1903 mL | 4.3806 mL | 10.9515 mL | |
| 10 mM | 0.2190 mL | 1.0951 mL | 2.1903 mL | 5.4757 mL | |
| 15 mM | 0.1460 mL | 0.7301 mL | 1.4602 mL | 3.6505 mL | |
| 20 mM | 0.1095 mL | 0.5476 mL | 1.0951 mL | 2.7379 mL | |
| 25 mM | 0.0876 mL | 0.4381 mL | 0.8761 mL | 2.1903 mL | |
| 30 mM | 0.0730 mL | 0.3650 mL | 0.7301 mL | 1.8252 mL | |
| 40 mM | 0.0548 mL | 0.2738 mL | 0.5476 mL | 1.3689 mL |