Catalog No.: PC-49026Not For Human Use, Lab Use Only.
ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.
ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.
ASP1126 selectively stimulated hS1P1 (EC50=13.4 uM) over hS1P3 (EC50=1760 nM) in Ca2+ influx assays.
ASP1126 has similar selectivity and agonistic activity for rat S1P1.
ASP1126 and tacrolimus synergistically prolong allograft survival in rats and monkeys.
ASP1126 decreased the number of peripheral lymphocytes, repeated dosing showed a cumulative effect on lymphopenia in both rats and monkeys.
ASP1126 reduced not only the number of naive T cells and central memory T cells but also effector memory T cells in the peripheral blood, and prolonged allograft survival in combination with tacrolimus in nonhuman primate (NHP) renal transplantation.
