HCAR1 Agonist

3-Chloro-5-hydroxybenzoic acid is a potent, orally active and selective lactate receptor GPR81 agonist, with an EC₅₀ of 16 μM for human GPR81. 3-Chloro-5-hydroxybenzoic acid exhibits favorable in vivo effects on lipolysis in a mouse model of obesity.

3-Hydroxybenzoic acid is an orally active endogenous metabolite. 3-Hydroxybenzoic acid is an agonist for GPR81 and GPR109A. 3-Hydroxybenzoic acid acts as stress response desensitizers. 3-Hydroxybenzoic acid can be used for anti-inflammatory and analgesic study.

3,5-Dihydroxybenzoic acid a potential biomarker for the consumption of many food products, including beer, nuts, peanut, and pulses. 3,5-Dihydroxybenzoic acid is the agonist for hydroxycarboxylic acid receptor 1 (HCA1, also known as GPR81) that inhibits lipolysis in adipocytes. 3,5-Dihydroxybenzoic acid is the competitive inhibitor for tyrosine phenol-lyase (TPL), exhibits an affinity of K_i=25.7 μM. 3,5-Dihydroxybenzoic acid is orally active.

GPR81 agonist 2 is a GPR81 agonist with an EC₅₀ of 0.023 μM for the human receptor. GPR81 agonist 2 activates the lactate-sensing receptor GPR81, inhibits forskolin-stimulated cAMP production and GTP binding of G_i protein. GPR81 agonist 2 can be used for research on type 2 diabetes.