AUY954

AUY954 is an orally bioavailable and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P₁; EC₅₀ = 1.2 nM for stimulating GTPγS binding to S1P₁ in CHO cells).¹ It is highly selective for the S1P₁ receptor with EC₅₀ values of >10,000, 1,210, >1,000, and 340 nM for S1P₂, S1P₃, S1P₄, and S1P₅ receptors, respectively. AUY954 reduces circulating lymphocytes and prevents rejection of rat heart allografts. In a rat model of experimental autoimmune neuritis, chronic treatment with AUY954 (10 mg/kg), starting on the day of immunization, almost completely prevents peripheral paralysis.² In the same model, it also decreases T cell, B cell, and macrophage infiltration and perivascular demyelination in sciatic nerves.

WARNING This product is not for human or veterinary use.

1. Pan, S., Mi, Y., Pally, C., et al. A monoselective sphingoine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem. Biol. 13(11), 1227-1234 (2006).

2. Zhang, Z.Y., Zhang, Z., Zug, C., et al. AUY954, a selective S1P₁ modulator, prevents experimental autoimmune neuritis. J. Neuroimmunol. 216(1-2), 59-65 (2009).