Cayman Chemical TASP0277308 10mg
An S1P1 antagonist (IC50 = 4.2 nM); selective for S1P1 over S1P3, S1P4, and S1P5 (IC50s = >10,000, >10,000, and 8,756 nM, respectively); inhibits S1P-induced [35S]GTPγS binding and forskolin-induced cAMP production in HEK293 cells expressing human S1P1 (IC50s = 7.8 and 4.3 nM, respectively); inhibits S1P-induced migration of CHO cells expressing human S1P1 (IC50 = 18 nM); induces lymphopenia in mice at 100 mg/kg; reduces bone erosion in a mouse model of collagen-induced arthritis; intrathecal administration reduces flinching and guarding behaviors in a mouse model of cancer-induced bone pain at 3 or 10 nmol/animal