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JTE-013
Cayman Chemical Item Number 10009458
Description 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 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↗
Formal Name N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-hydrazinecarboxamide
CAS Number 383150-41-2
Molecular Formula C17H19Cl2N7O
Formula Weight 408.3
Formulation A crystalline solid
Purity ≥98%
λmax 216, 248, 304 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES O=C(NNc1cc(C(C)C)c2c(C)nn(C)c2n1)Nc1cc(Cl)nc(Cl)c1
InCHI Code 1S/C17H19Cl2N7O/c1-8(2)11-7-14(22-16-15(11)9(3)25-26(16)4)23-24-17(27)20-10-5-12(18)21-13(19)6-10/h5-8H,1-4H3,(H,22,23)(H2,20,21,24,27)
InCHI Key RNSLRQNDXRSASX-UHFFFAOYSA-N |