| Bioactivity | 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 | ||||||||||||
| Target | IC50: GPR109A (G-protein coupled receptor 109A); HCA2 (hydroxy-carboxylic acid receptor 2) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | GSK256073 (oral adminstration; 1, 30 and 100 mg/kg; in rat) shows that the fall in NEFA is of rapid onset and that the maximum is dose-related with inhibitions of 74, 81 and 88%, respectively. Triglycerides decrease is followed as a similar pattern,although the duration was longer with a decrease of 91% still present 6 h post dose at 10 mg/kg[2].GSK256073 (intravenous injection; 1-10 mg/kg) produces a dose related decrease in NEFA. However, the increase in ear temperature induced by 10 mg/kg i.v. GSK256073 is only 40% of that induced by 10 mg/kg i.v. niacin[2]. Animal Model: | ||||||||||||
| Name | GSK256073 | ||||||||||||
| CAS | 862892-90-8 | ||||||||||||
| Formula | C10H13ClN4O2 | ||||||||||||
| Molar Mass | 256.69 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. [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. |
GSK256073
CAS: 862892-90-8 F: C10H13ClN4O2 W: 256.69
GSK256073 is a potent, selective and orally active GPR109A agonist and a long-lasting and non-flushing HCA2 full agonist
Sales Email：peptidedb@qq.com
This product is for research use only, not for human use. We do not sell to patients.