| 货号 | 10009458-1mg |
| 描述 | Sphingosine-1-phosphate (S1P) is a bioactive lipid that exhibits a broad spectrum of biological activities including cell proliferation, survival, migration, cytoskeletal organization, and morphogenesis.1,2,3 It exerts its activity by binding to five distinct G protein-coupled receptors, S1P1/EDG-1, S1P2/EDG-5, S1P3/EDG-3, S1P4/EDG-6, and S1P5/EDG-8.1,2 JTE-013 is a potent, selective sphingosine-1-phosphate 2 (S1P2) receptor antagonist that binds to the human and rat receptors with IC50 values of 17 and 22 nM, respectively, (IC50 values >10 µM for human S1P1 and S1P3).4 It reverses the inhibitory effects of S1P on cell migration of vascular endothelial cells and smooth muscle cells. Similarly, JTE-013 reverses the inhibition of S1P on invasion and migration of B16 melanoma cells.4,5 JTE-013 inhibits S1P-induced contraction of, as well as cyclic AMP accumulation in, coronary artery smooth muscle cells.6,7 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Takuwa, Y.,Takuwa, N., and Sugimoto, N. The Edg family G protein-coupled receptors for lysophospholipids: Their signaling properties and biological activities. Journal of Biochemistry 131, 767-771 (2002). 2.Ishii, I.,Fukushima, N.,Ye, X., et al. Lysophospholipid receptors: Signaling and biology. Annual Reviews of Biochemistry 73, 321-354 (2004). 3.Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochimica et Biophysica Acta 1582, 72-80 (2002). 4.Osada, M.,Yatomi, Y.,Ohmori, T., et al. Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist. Biochemical and Biophysical Research Communications 299, 483-487 (2002). 5.Arikawa, K.,Takuwa, N.,Yamaguchi, H., et al. Ligand-dependent inhibition of B16 melanoma cell migration and invasion via endogenous S1P2 G protein-coupled receptor. Requirement of inhibition of cellular rac activity. The Journal of Biological Chemisty 278(35), 32841-32851 (2003). 6.Damirin, A.,Tomura, H.,Komachi, M., et al. Sphingosine 1-phosphate receptors mediate the lipid-induced cAMP accumulation through cyclooxygenase-2/prostaglandin I2 pathway in human coronary artery smooth muscle cells. Molecular Pharmacology 67(4), 1177-1185 (2005). 7.Ohmori, T.,Yatomi, Y.,Osada, M., et al. Sphingosine 1-phosphate induces contraction of coronary artery smooth muscle cells via S1P2. Cardiovascular Research 58, 170-177 (2003). | |
| 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 | 408.3 |
| 分子式 | C17H19Cl2N7O |
| CAS号 | 383150-41-2 |
| 稳定性 | ≥ 2 years |
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