| CAS NO: | 53984-36-4 |
| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 500mg | 电议 |
| Storage | Store at -20°C |
| M.Wt | 172.6 |
| Cas No. | 53984-36-4 |
| Formula | C7H5ClO3 |
| Synonyms | 3-chloro-5-hydroxy BA,CHBA,GPR81 Agonist |
| Solubility | insoluble in H2O; ≥52.2 mg/mL in EtOH; ≥6.65 mg/mL in DMSO |
| Chemical Name | 3-chloro-5-hydroxy-benzoic acid |
| Canonical SMILES | ClC1=CC(O)=CC(C(O)=O)=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
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