Hydroxycarboxylic Acid Receptor (HCAR)

The hydroxycarboxylic acid (HCA) receptor family consists of three members, HCA1, HCA2, and HCA3, also known as GPR81, GPR109A, and GPR109B, respectively, which are encoded by closely related genes. The physiological ligands of HCA receptors are key metabolic intermediates whose local and systemic levels reflect particular metabolic states. Lactic acid, the end product of glycolysis, activates HCA1, whereas the ketone body 3-hydroxy-butyric acid [b-hydroxybutyrate (b-HB)] and the b-oxidation intermediate 3-hydroxy-octanoic acid activate HCA2 and HCA3, respectively. In addition, HCA2 is also activated by butyric acid. All three HCA receptors are highly expressed in white and brown adipocytes. Expressions of HCA1 and HCA2 have been shown to increase during differentiation of adipocytes from preadipocytes as well as after activation of peroxisome proliferator-activated receptor-gamma. Both high-fat diet (HFD) feeding and exposure to various inflammatory stimuli result in decreased expression of HCA1 in the adipose tissue. While HCA2 expression in the adipose tissue is also decreased after HFD feeding, inflammatory stimuli increase expression of HCA2. During the past decade, it has become clear that HCA receptors help to maintain homeostasis under changing metabolic and dietary conditions, by controlling metabolic, immune, and other body functions. Work based on genetic mouse models and synthetic ligands of HCA receptors has, in addition, shown that members of this receptor family can serve as targets for the prevention and therapy of diseases such as metabolic and inflammatory disorders.

Hydroxycarboxylic Acid Receptor (HCAR) Related Products (5):

By Effects:	Inhibitors (2) Agonists (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-135982

GPR81 agonist 1	Inhibitor	99.73%
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC₅₀s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.

HY-W016868

3-Chloro-5-hydroxybenzoic acid	Agonist	99.54%
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.

HY-100976

LUF6283	Agonist	≥99.0%
LUF6283 is a potent and orally active HCA(2) partial agonist, with a K_i of 0.55 µM. LUF6283 can achieve the beneficial lipid lowering effect of niacin without producing the unwanted cutaneous flushing side effect.

HY-141434

5-OxoETE methyl ester	Agonist
5-OxoETE methyl ester is the agonist for oxoeicosanoid receptor 1 (OXER1). 5-OxoETE methyl ester binds to OXER1, and activates downstream signaling pathways β-arrestin recruitment with an EC₅₀ of 1.54 µM.

HY-148563

GPR81 agonist 2	Inhibitor
GPR81 agonist 2 (compound 1) is a potent GPR81 agonist with EC₅₀ values of 0.023, 0.123 µM for hGPR81, hGPR109A, respectively.

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