GSK256073

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

Product Specifications

CAS Number

[862892-90-8]

Product Name Alternative

BafA1

UNSPSC

12352005

Hazard Statement

H302, H361

Target

GPR109A

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Assay Protocol

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

Concentration

10mM

Purity

99.39

Solubility

DMSO : 16.67 mg/mL (ultrasonic)

Smiles

O=C(N(C1=C2NC(Cl)=N1)CCCCC)NC2=O

Molecular Formula

C10H13ClN4O2

Molecular Weight

256.69

Precautions

H302, H361

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.