GSK256073

GSK256073

Identifiers
IUPAC name 8-chloro-3-pentyl-7H-purine-2,6-dione
CAS Number	862892-90-8
PubChem CID	46215799
IUPHAR/BPS	8470
ChemSpider	35033254
UNII	1VI94C980K
ChEMBL	ChEMBL3730241
Chemical and physical data
Formula	C10H13ClN4O2
Molar mass	256.69 g·mol−1
3D model (JSmol)	Interactive image
SMILES CCCCCN1C2=C(C(=O)NC1=O)NC(=N2)Cl
InChI InChI=1S/C10H13ClN4O2/c1-2-3-4-5-15-7-6(12-9(11)13-7)8(16)14-10(15)17/h2-5H2,1H3,(H,12,13)(H,14,16,17) Key:CGAMDQCXAAOFSR-UHFFFAOYSA-N

GSK256073 is an experimental drug which acts as a potent and selective agonist for the Hydroxycarboxylic acid receptor 2 (GPR109A). It reduces blood sugar levels and was trialed unsuccessfully as a potential treatment for diabetes, but continues to be used for research into the function of the HCA2 receptor. ^{[1] [2] [3] [4] [5]}

References

1. Dobbins RL, Shearn SP, Byerly RL, Gao FF, Mahar KM, Napolitano A, et al. (November 2013). "GSK256073, a selective agonist of G-protein coupled receptor 109A (GPR109A) reduces serum glucose in subjects with type 2 diabetes mellitus". Diabetes, Obesity & Metabolism. 15 (11): 1013–1021. doi:10.1111/dom.12132. PMID   23701262.
2. Dobbins R, Byerly R, Gaddy R, Gao F, Mahar K, Napolitano A, et al. (May 2015). "GSK256073 acutely regulates NEFA levels via HCA2 agonism but does not achieve durable glycaemic control in type 2 diabetes. A randomised trial". European Journal of Pharmacology. 755: 95–101. doi: 10.1016/j.ejphar.2015.03.005 . PMID   25773496.
3. Sprecher D, Maxwell M, Goodman J, White B, Tang CM, Boullay V, et al. (June 2015). "Discovery and characterization of GSK256073, a non-flushing hydroxy-carboxylic acid receptor 2 (HCA2) agonist". European Journal of Pharmacology. 756: 1–7. doi:10.1016/j.ejphar.2015.01.051. PMID   25773497.
4. Zhu S, Yuan Q, Li X, He X, Shen S, Wang D, et al. (November 2023). "Molecular recognition of niacin and lipid-lowering drugs by the human hydroxycarboxylic acid receptor 2". Cell Reports. 42 (11) 113406. doi: 10.1016/j.celrep.2023.113406 . PMID   37952153.
5. Richardson JC, Higgins GA, Upton N, Massey P, Cunningham M, Wilson S, et al. (December 2024). "The hydroxycarboxylic acid receptor HCA2 is required for the protective effect of ketogenic diet in epilepsy". Pharmacology Research & Perspectives. 12 (6) e70026. doi:10.1002/prp2.70026. PMC   11496569 . PMID   39439218.