GPR109 receptor agonist-1

GPR109 receptor agonist-1 is a highly selective agonist of the human orphan G protein-coupled receptor GPR109b, and does not activate the mouse homologous receptor PUMA-G. GPR109 receptor agonist-1 functionally modulates the human GPR109b receptor via the cAMP signaling pathway, with an EC₅₀ of 400 nM. GPR109 receptor agonist-1 inhibits isoproterenol (HY-B0468)-stimulated lipolysis in human subcutaneous adipocytes, with efficacy comparable to that of Niacin (HY-B0143), and does not act on β-adrenergic receptors. GPR109 receptor agonist-1 can be used in studies related to dyslipidemia and atherosclerosis^[1]. IC50 & Target:pEC₅₀: 6.40 ± 0.36 (GPR109b)^[1] In Vitro:GPR109 receptor agonist-1 (compound 3a) (30 pM-100 μM) completely reverses the cAMP elevation effect of Forskolin (HY-15371), and shows no significant activity against the highly homologous GPR109a receptor and non-transfected control cells at a concentration of 1 mM^[1].
GPR109 receptor agonist-1 (1-100 nM) dose-dependently inhibits isoproterenol (HY-B0468)-stimulated lipolysis in human cadaveric subcutaneous adipocytes, with efficacy comparable to that of Niacin (HY-B0143), and does not act on β-adrenergic receptors^[1].