| 货号 | 12046-50mg |
| 描述 | GPR35 is a G protein-coupled receptor that is activated by kynurenic acid and 2-acyl lysophosphatidic acids (e.g., 2-oleoyl lysophosphatidic acid).1,2,3 It is expressed predominantly on immune cells, the brain, and in the gastrointestinal tract.4,2 GPR35 is overexpressed in gastric cancer cells.5 CID-2745687 is a reversible, competitive antagonist of GPR35, blocking activation by the synthetic agonist pamoic acid with a Ki value of 12.8 nM.6 It less potently blocks activation of GPR35 by zaprinast (Item No. 10010421) (IC50 = 160 nM).7 It shows ~57-fold selectivity for GPR35 over the related receptor GPR55 (IC50 = 9.08 µM).7 |
| 别名 | ML-194; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Oka, S.,Ota, R.,Shima, M., et al. GPR35 is a novel lysophosphatidic acid receptor. Biochemical and Biophysical Research Communications 395(2), 232-237 (2010). 2.Wang, J.,Simonavicius, N.,Wu, X., et al. Kynurenic acid as a ligand for orphan G protein-coupled receptor GPR35. The Journal of Biological Chemisty 281(31), 22021-22028 (2006). 3.MacKenzie, A.E.,Lappin, J.E.,Taylor, D.L., et al. GPR35 as a novel therapeutic target. Front.Endocrinol.(Lausanne) 2, 68 (2011). 4.ODowd, B.F.,Nguyen, T.,Marchese, A., et al. Discovery of three novel G-protein-coupled receptor genes. Genomics 47, 310-313 (1998). 5.Okumura, S.i.,Baba, H.,Kumada, T., et al. Cloning of a G-protein-coupled receptor that shows an activity to transform NIH3T3 cells and is expressed in gastric cancer cells. Cancer Science 95(2), 131-135 (2004). 6.Zhao, P.,Sharir, H.,Kapur, A., et al. Targeting of the orphan receptor GPR35 by pamoic acid: A potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Molecular Pharmacology 78(4), 560-568 (2010). 7.Heynen-Genel, S.,Dahl, R.,Shi, S., et al. Selective GPR35 antagonists: Antagonists for the orphan receptor GPR35. Probe 3, 1-18 (2011). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 395.4 |
| 分子式 | C17H19F2N5O2S |
| CAS号 | 264233-05-8 |
| 稳定性 | ≥ 2 years |
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