862892-90-8
862892-90-8
Chemical Structure
GSK256073
- CAS No.: 862892-90-8
- Formula:C10H13ClN4O2
- Molecular Weight:256.69
IUPAC Name: 8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione
InChIKey: CGAMDQCXAAOFSR-UHFFFAOYSA-N
SMILES: O=C(N(C1=C2NC(Cl)=N1)CCCCC)NC2=O
Biological Activity: 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[1][2]. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2
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GSK256073 | 99.39% | 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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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]
