GSK256073
Based on 3 publication(s) in Google Scholar
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist with a pEC50 of 7.5 (human HCA2). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis and has the potential for the study of type 2 diabetes mellitus (T2DM)and dyslipidemia. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
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- Purity: 99.39%
- CAS No.: 862892-90-8
- 화학식: C10H13ClN4O2
- 분자량:256.69
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) GSK256073
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Biological Activity
IC50: GPR109A (G-protein coupled receptor 109A); HCA2 (hydroxy-carboxylic acid receptor 2)[1][2]
GSK256073 is approximately 10-fold more potent than niacin against human HCA2 (pEC50 value of 7.5 compared to 6.7 for niacin), has good activity versus the rat orthologue of HCA2 (pEC50 value of 6.9 compared to 6.4 for niacin) in membranes prepared from Chinese hamster ovary cellsexpressing recombinant human HCA2[2].GSK256073 (100 μM) suppresses cAMP elevation induced by isoprenaline (100 nM) in rat primary adipocytes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rat[2]
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Dosage:1, 30 and 100 mg/kg
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Administration:Oral adminstration
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Result:Inhibited NEFA expression as a dose-dependent manner.
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Animal Model:Guinea pigs[2]
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Dosage:10 mg/kg
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Administration:Intravenous injection
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Result:Had the antilipolytic and flushing effects as a HCA2 agonist.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 862892-90-8
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Appearance Solid
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분자량 256.69
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화학식 C10H13ClN4O2
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Color White to off-white
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SMILES
O=C(N(C1=C2NC(Cl)=N1)CCCCC)NC2=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Fusobacterium nucleatum facilitates anti-PD-1 therapy in microsatellite stable colorectal cancer. [Abstract]2024 Oct 14;42(10):1729-1746.e8. PMID: 39303724 -
iScience
Comparative analysis reveals molecular adaptation of mammalian HCA2 to microbial metabolites. [Abstract]2026 May 22;29(6):116030. PMID: 42221821 -
용액&용해도
DMSO : 16.67 mg/mL (64.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
순도&문서
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Data Sheet (276 KB)
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SDS (556 KB)
- English - EN (556 KB)
- Français - FR (556 KB)
- Deutsch - DE (556 KB)
- Norwegian - NO (556 KB)
- Español - ES (556 KB)
- Swedish - SV (556 KB)
- Italian - IT (556 KB)
- Korean - KR (556 KB)
- Portuguese - PT (556 KB)
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Handling Instructions (2659 KB)
References
[1]. Dobbins RL, et al. GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus.Diabetes Obes Metab. 2013 Nov;15(11):1013-21. [Content Brief]
[2]. Sprecher D, et al. Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist.Eur J Pharmacol. 2015 Jun 5;756:1-7. [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 | 3.8957 mL | 19.4787 mL | 38.9575 mL | 97.3937 mL |
| 5 mM | 0.7791 mL | 3.8957 mL | 7.7915 mL | 19.4787 mL | |
| 10 mM | 0.3896 mL | 1.9479 mL | 3.8957 mL | 9.7394 mL | |
| 15 mM | 0.2597 mL | 1.2986 mL | 2.5972 mL | 6.4929 mL | |
| 20 mM | 0.1948 mL | 0.9739 mL | 1.9479 mL | 4.8697 mL | |
| 25 mM | 0.1558 mL | 0.7791 mL | 1.5583 mL | 3.8957 mL | |
| 30 mM | 0.1299 mL | 0.6493 mL | 1.2986 mL | 3.2465 mL | |
| 40 mM | 0.0974 mL | 0.4870 mL | 0.9739 mL | 2.4348 mL | |
| 50 mM | 0.0779 mL | 0.3896 mL | 0.7791 mL | 1.9479 mL | |
| 60 mM | 0.0649 mL | 0.3246 mL | 0.6493 mL | 1.6232 mL |
GSK256073 Related Classifications
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