ДЖТЕ-013

Описание

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. 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. 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). 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. JTE-013 inhibits S1P-induced contraction of, as well as cyclic AMP accumulation in, coronary artery smooth muscle cells.

Использование

JTE-013 has been used in in vitro blood?brain barrier (BBB) and blood?tumor barrier (BTB) assays.

Биохимия/физиол Действия

JTE-013 can enhance the excitability of small-diameter sensory neurons. It has the ability to repress sphingosine 1-phosphate (S1P)-mediated cellular migration.