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You are here:Home-Inhibitors & Agonists-GPCR-GPR109A (Niacin Receptor 1)

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GPR109A is a G-protein-coupled receptor for nicotinate but recognizes butyrate with low affinity. GPR109A is expressed in the lumen-facing apical membrane of colonic and intestinal epithelial cells and that the receptor recognizes butyrate as a ligand. The expression of GPR109A is silenced in colon cancer in humans, in a mouse model of intestinal/colon cancer, and in colon cancer cell lines. The tumor-associated silencing of GPR109A involves DNA methylation directly or indirectly. Reexpression of GPR109A in colon cancer cells induces apoptosis, but only in the presence of its ligands butyrate and nicotinate. Butyrate is an inhibitor of histone deacetylases, but apoptosis induced by activation of GPR109A with its ligands in colon cancer cells does not involve inhibition of histone deacetylation. The primary changes in this apoptotic process include down-regulation of Bcl-2, Bcl-xL, and cyclin D1 and up-regulation of death receptor pathway. In addition, GPR109A/butyrate suppresses nuclear factor-kappaB activation in normal and cancer colon cell lines as well as in normal mouse colon. These studies show that GPR109A mediates the tumor-suppressive effects of the bacterial fermentation product butyrate in colon.

Cat. No. Product Name CAS No. Information
H9149

GSK256073

 		862892-90-8

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. GPR109A: G-protein coupled receptor 109A; HCA2: hydroxy-carboxylic acid receptor 2.
H3360

MK-6892

 		917910-45-3

A potent and selective high affinity niacin receptor (GPR109A) full agonist with Ki of 4.0 nM, EC50 of 16 nM in GTPγS assay; has no activity on closely related GPCRs GPR109B and GPR81; displays good PK across species, remarkably clean off-target profiles, and superior therapeutic window over niacin regarding the FFA reduction versus vasodilation in rats and dogs.
H3359

MK-0354

 		851776-28-8

MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays; shows no interaction with any other target in a panel of over 120 other proteins; MK-0354 is a competitive inhibitor of 3H-nicotinic acid binding to hGPR109a with Ki of 505 nM, fully inhibits isoproterenol stimulated lipolysis in human adipocytes with IC50 of 3.1 uM, also is a competitive antagonist of nicotinic acid-induced MAPK signaling in cells overexpressing either mGPR109a or hGPR109a; possesses plasma FFA lowering effects in mice comparable to those of nicotinic acid, does not induce vasodilation.

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