GSK256073 (tris)

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

Product Specifications

CAS Number

[1228650-42-7]

UNSPSC

12352005

Target

GPR109A

Type

Reference compound

Related Pathways

GPCR/G Protein

Field of Research

Metabolic Disease

Assay Protocol

https://www.medchemexpress.com/gsk256073-tris.html

Smiles

O=C1NC(N(CCCCC)C2=C1NC(Cl)=N2)=O.OCC(CO)(CO)N

Molecular Formula

C14H24ClN5O5

Molecular Weight

377.82

References & Citations

[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.