gpr109

GPR109 receptor agonist-3 is an orally active GPR109 receptor agonist with an IC50 of 310 nM. It retains the antioxidant and cytoprotective properties of lipoic acid. In rats on a high-fat diet, GPR109 receptor agonist-3 reduces total cholesterol (TC), triglycerides (TG), and low-density lipoprotein cholesterol (LDL-C), while increasing high-density lipoprotein cholesterol (HDL-C). This compound is applicable for atherosclerosis research.

Compound 5, a selective GPR109a agonist, exhibits a pEC50 value of 5.53 [1].

Benzyl nicotinate (Pycaril) is a agonist of GPR109A receptor and GPR109B receptor

IBC 293 is selective for GPR109B over niacin receptor GPR109A. IBC 293 is a highly selective agonist for GPR109B, a human orphan G-protein-coupled receptor expressed in adipocytes.

Mepenzolate Bromide (Colibantil) is a muscarinic antagonist used to treat gastrointestinal conditions.

Monomethyl fumarate is a potent agonist of GPR109A .

Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug being developed for delivering nicotinic acid (NIC) into the skin to prevent actinic keratosis and its progression to skin cancer.

Lactic acid (2-hydroxypropanoic acid), a glycolysis end product, is a hydroxycarboxylic acid receptor 1 (HCAR1) activator (EC50=4.2-5 mM). Lactic acid can be used as a hemodynamic index in critically ill patients and has anti-tumor activity.

D-Kynurenine (ZINC901103) is a metabolite of D-tryptophan and an agonist of GPR109B. D-Kynurenine activates AhR and promotes the conversion of the epithelium to mesenchyme. D-Kynurenine serves as a substrate in the fluorescence analysis of D-amino acid oxidase.

GSK256073 is an orally active GPR109A agonist. GSK256073 also is a long-lasting and non-flushing HCA2 (hydroxy-carboxylic acid receptor 2) full agonist (pEC50: 7.5). GSK256073 acutely improves glucose homeostasis via inhibition of lipolysis.

Acifran (AY 25712) is an HM74A/GPR109A and GPR109B agonist and displays antihyperlipidemic activity.

MK 1903 is a potent and selective complete agonist for the hydroxy-carboxylic acid receptor 2 (HCA2). HCA2 is also known as G protein-coupled receptor 109A(GPR109A). MK 1903 reduced Foschlin-induced cAMP production in uniform time-resolved fluorescence (htf) measurements using CHO cells expressing the human receptor (ECso-12.9 nM).

GPCR agonist-2 (4-(Cyclopropylamino)-3-nitrobenzoic acid) is an agonist of the orphan human GPCR GPR109B.

3-Hydroxyoctanoic Acid is one of the hydroxy-carboxylic acids (HCAs) that serve as intermediates of energy metabolism. It is an agonist of the orphan receptor GPR109B.

MK-6892 is a selective and full agonist for the high-affinity nicotinic acid receptor GPR109A (Ki: 4 nM; GTPγS EC50: 16 nM).