| Identification | Back Directory | [Name]
8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxylmethyl)aminomethane salt | [CAS]
1228650-42-7 | [Synonyms]
8-chloro-3-pentyl-3,7-dihydro-1H-purine-2,6-dione tris(hydroxylmethyl)aminomethane salt | [Molecular Formula]
C14H24ClN5O5 | [MDL Number]
MFCD30489254 | [MOL File]
1228650-42-7.mol | [Molecular Weight]
377.83 |
| Hazard Information | Back Directory | [Description]
GSK256073 is an agonist of G-protein coupled receptor 109A (GPR109A). It acts by reducing serum glucose in subjects with type 2 diabetes mellitus. | [Uses]
GSK256073 tris 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 tris 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 | [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. DOI:10.1111/dom.12132
[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. DOI:10.1016/j.ejphar.2015.01.051 |
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