Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: N-(2,6-dichloro-4-pyridinyl)-2-[1,3-dimethyl-4-(1-methylethyl)-1H-pyrazolo[3,4-b]pyridin-6-yl]-hydrazinecarboxamide
Purity: ≥98%
Formula Markup: C17H19Cl2N7O
Formula Weight: 408.3
CAS Number: 383150-41-2
Notes: JTE-013 is a sphingosine-1-phosphate receptor 2 (S1P2) and S1P4 antagonist (IC50s = 17 and 237 nM, respectively).{61853} It is selective for S1P2 over S1P1 and S1P3 (IC50s = >10 µM for both).{61853,14560} JTE-013 (1 and 10 µM) reverses S1P-induced inhibition of human umbilical vein endothelial cell (HUVEC) and smooth muscle cell (SMC) migration.{14560} It also reverses S1P-induced inhibition of B16 murine melanoma cell migration.{14559} In vivo, JTE-013 (30 mg/kg) reduces lung injury, endothelial dysfunction, and pulmonary edema in a rat model of cecal ligation and puncture-induced sepsis.{61854} JTE-013 also inhibits sphingolipid delta(4)-desaturase (DES1; IC50 = 16.8 µM), an effect that is not rescued by the S1P2 agonist CYM5520, as well as sphingosine kinase 1 (SK1) and SK2 (IC50s = 25.1 and 4.3 µM, respectively).{61853}
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