3-chloro-5-hydroxy BA

GPR81, also known as hydroxycarboxylic acid receptor 1 (HCAR1), is a recently de-orphanized receptor that is activated by lactic acid (EC₅₀ ~ 1.5 mM) but not by other hydroxycarboxylic acids.^1,2 3-chloro-5-hydroxy BA is an agonist of GPR81 (EC₅₀ = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor.³ It is similarly effective at GPR81 receptors from a variety of mammalian species and is bioavailable, stimulating lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks.³ 3-chloro-5-hydroxy BA, like lactate, blocks basal ghrelin secretion by primary gastric mucosal cells.⁴

WARNING This product is not for human or veterinary use.

1. Ahmed, K., Tunaru, S., and Offermanns, S. GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors. Trends Pharmacol. Sci. 30(11), 557-562 (2009).

2. Davenport, A.P., Alexander, S.P.H., Sharman, J.L., et al. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands. Pharmacol. Rev. 65(3), 967-986 (2013).

3. Dvorak, C.A., Liu, C., Shelton, J., et al. Identification of hydroxybenzoic acids as selective lactate receptor (GPR81) agonists with antilipolytic effects. ACS Med. Chem. Lett. 3(8), 637-639 (2012).

4. Engelstoft, M.S., Park, W.m., Sakata, I., et al. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol. Metab. 2(4), 376-392 (2013).