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.
CAS：909725-62-8
分子式：C16H27N2O4P.CF3COOH
分子量：456.4
纯度：98%
存储：Store at -20°C

Background:

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. W146 is a S1P1 receptor antagonist that exhibits a Ki value of 77 nM for the human receptor in a GTP-γS binding assay with equipotency at the murine S1P1 receptor (2a = W146; 2b = W140 in supplemental material). [4] No agonist or antagonist activity was observed at 10 &#181M W146 at S1P2, S1P3, or S1P5 receptors. W146 is active in vivo causing skin capillary leakage in murine lung and skin as well as inhibition of S1P1 agonist-induced lymphocyte sequestration. The half-life of W146 in rat blood is 73 minutes.

Reference:
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[3]. Kluk, M.J., and Hla, T. Signaling of sphingosine-1-phosphate via the S1P/EDG-family of G-protein-coupled receptors. Biochim. Biophys. Acta 1582(1-3), 72-80 (2002).
[4]. Sanna, M.G., Wang, S.K., Gonzalez-Cabrera, P.J., et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nature Chemical Biology 2(8), 434-441 (2006).