Catalog No.: PC-21439Not For Human Use, Lab Use Only.
GSK256073 is a highly potent, selective agonist of hydroxy-carboxylic acid receptor 2 (HCA2, HM74A/GPR109A) with pEC50 of 7.5, 100-fold selective over HCA3 (pEC50=5.6).
GSK256073 is a highly potent, selective agonist of hydroxy-carboxylic acid receptor 2 (HCA2, HM74A/GPR109A) with pEC50 of 7.5, 100-fold selective over HCA3 (pEC50=5.6). GSK256073 is a full and potent agonist (pEC50=6.48) at human adipocyte membranes using a [35S]GTP-γS binding assay. GSK256073 does not display significant activity against a number of 7-transmembrane receptors, ion channels, transporters, and phophodiesterases. GSK256073 (0.03, 0.3, 3.0 and 30 mg/kg) inhibited triglyceride accumulation by 7%, 30%, 51% and 78%, respectively, in rats.
Physicochemical Properties
M.Wt
256.69
Formula
C10H13ClN4O2
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
8-chloro-3-pentyl-7H-purine-2,6-dione
References
1. Sprecher D, et al. Eur J Pharmacol. 2015 Jun 5;756:1-7.
2. Dobbins R, et al. Eur J Pharmacol. 2015 May 15;755:95-101.
