| 货号 | 16795-25mg |
| 描述 | GPR81, also known as hydroxycarboxylic acid receptor 1 (HCAR1), is a recently de-orphanized receptor that is activated by lactic acid (EC50 ~ 1.5 mM) but not by other hydroxycarboxylic acids.1,2 3-chloro-5-hydroxy Benzoic Acid (3-chloro-5-hydroxy BA) is an agonist of GPR81 (EC50 = 16 µM) that is inactive against the related GPR109a (HCAR2) receptor.3 It is similarly effective at GPR81 receptors from a variety of mammalian species and is bioavailable, stimulating lipolysis (increased serum free fatty acids) in mice fed high fat chow for 10 weeks.3 3-chloro-5-hydroxy BA, like lactate, blocks basal ghrelin secretion by primary gastric mucosal cells.4 |
| 别名 | 3-chloro-5-hydroxy BA;CHBA;GPR81 Agonist; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ahmed, K.,Tunaru, S. and Offermanns, S. GPR109A, GPR109B and GPR81, a family of hydroxy-carboxylic acid receptors. Trends in Pharamacological Sciences 30(11), 557-562 (2009). 2.Davenport, A.P.,Alexander, S.P.H.,Sharman, J.L., et al. International Union of Basic and Clinical Pharmacology. LXXXVIII. G protein-coupled receptor list: Recommendations for new pairings with cognate ligands. Pharmacological Reviews 65(3), 967-986 (2013). 3.Dvorak, C.A.,Liu, C.,Shelton, J., et al. Identification of hydroxybenzoic acids as selective lactate receptor (GPR81) agonists with antilipolytic effects. ACS Med.Chem.Lett. 3(8), 637-639 (2012). 4.Engelstoft, M.S.,Park, W.m.,Sakata, I., et al. Seven transmembrane G protein-coupled receptor repertoire of gastric ghrelin cells. Mol.Metab. 2(4), 376-392 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 172.6 |
| 分子式 | C7H5ClO3 |
| CAS号 | 53984-36-4 |
| 稳定性 | ≥ 2 years |
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