NVP-AUY954 is an orally-available, benzothiazole-based, monoselective agonist of the sphingosine-1-phosphate receptor 1 (S1P1) intended for the treatment of human autoimmune mediated inflammatory neuropathies. Along with EC50 potency of 1.2 nM, NVP-AUY954 has at least 280-fold selectivity for S1P1 compared to the receptor's four other subtypes. (1, 2)

NVP-AUY954 induces a potent and reversible reduction of circulating lymphocytes; in combination with Everolimus, NVP-AUY954 can prolong the survival of cardiac allografts in a rat transplantation model. NVP-AUY954 also has been shown to activate downstream kinase cascades, increasing Erk (Tyr204) and Akt (Ser473) phosphorylation at EC50s of 0.1 and 1.0 nM, respectively. (2)

NVP-AUY954 efficacy has been correlated with an accumulation of plasmacytoid dendritic cells (pDC), which may have therapeutic value in the treatment of multiple sclerosis. (3)

NVP-AUY954 is an orally-available, benzothiazole-based, monoselective agonist of the sphingosine-1-phosphate receptor 1 (S1P1) intended for the treatment of human autoimmune mediated inflammatory neuropathies. Along with EC50 potency of 1.2 nM, NVP-AUY954 has at least 280-fold selectivity for S1P1 compared to the receptor's four other subtypes. (1, 2)

NVP-AUY954 induces a potent and reversible reduction of circulating lymphocytes; in combination with Everolimus, NVP-AUY954 can prolong the survival of cardiac allografts in a rat transplantation model. NVP-AUY954 also has been shown to activate downstream kinase cascades, increasing Erk (Tyr204) and Akt (Ser473) phosphorylation at EC50s of 0.1 and 1.0 nM, respectively. (2)

NVP-AUY954 efficacy has been correlated with an accumulation of plasmacytoid dendritic cells (pDC), which may have therapeutic value in the treatment of multiple sclerosis. (3)