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3-chloro-5-hydroxy BA

Catalog No.
GPR81 agonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
In stock
In stock
In stock

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3-chloro-5-hydroxy BA is a GPR81 agonist.

GPR81 (HCA1) is a member of G-protein-coupled receptors (GPCRs). GPR81 is predominantly expressed on adipocytes and is activated by the endogenous ligands 2-hydroxypropanoate (lactate). Stimulation of GPR81 in adipose tissue lead to a decrease in the lipolysis of triglycerides by hormone-sensitive lipase, which resulted in reduced transport of fatty acids to the liver and a decrease in hepatic triglycerides [1].

In vitro: In the hGPR81 assay, 3-chloro-5-hydroxybenzoic acid showed the potency against GPR81 with an EC50 of 16 μM. The EC50 of 3-chloro-5-hydroxybenzoic acid against monkey GPR81, dog GPR81, rat GPR81, mouse GPR81, and hamster GPR81 was 17 μM, 67 μM, 7 μM, 22 μM and 27 μM, respectively [1]. 3-chloro-5-hydroxy BA blocked basal ghrelin secretion by primary gastric mucosal cells [2].

In vivo: In mice, oral administration of 3-chloro-5-hydroxybenzoic acid at 30 mg/kg provided a Cmax of 67 μM at approximately 3-fold over the in vitro EC50 with an AUCinf of 54 h μM and a short t1/2 of 1.5 h, and the 100 mg/kg p.o dose attained a Cmax of 342 μM at greater than 15-fold over the observed in vitro EC50 [1].

[1].  Dvorak C A, Liu C, Shelton J, et al. Identification of hydroxybenzoic acids as selective lactate receptor (GPR81) agonists with antilipolytic effects[J]. ACS medicinal chemistry letters, 2012, 3(8): 637-639.
[2].  Engelstoft M S, Park W, Sakata I, et al. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells[J]. Molecular metabolism, 2013, 2(4): 376-392.

Chemical Properties

StorageStore at -20°C
Cas No.53984-36-4
Synonyms3-chloro-5-hydroxy BA,CHBA,GPR81 Agonist
Solubility≥6.65mg/mL in DMSO
Chemical Name3-chloro-5-hydroxy-benzoic acid
SDFDownload SDF
Canonical SMILESClC1=CC(O)=CC(C(O)=O)=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

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