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3-chloro-5-hydroxy BA
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
3-chloro-5-hydroxy BA图片
CAS NO:53984-36-4
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议
100mg电议
500mg电议

产品介绍
3-chloro-5-hydroxy BA 是一种有效的、具有口服活性的选择性乳酸受体 GPR81 激动剂，对人 GPR81 的 EC50 为 16 μM。
Cas No.53984-36-4
别名3-氯-5-羟基苯甲酸,3-chloro-5-hydroxy BA,CHBA,GPR81 Agonist
化学名3-chloro-5-hydroxy-benzoic acid
Canonical SMILESClC1=CC(O)=CC(C(O)=O)=C1
分子式C7H5ClO3
分子量172.6
溶解度≥ 6.65mg/mL in DMSO
储存条件Store at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.