AUY954

AUY954 is a potent, orally active, and highly selective small molecule agonist of the **sphingosine-1-phosphate receptor 1 (S1PR1)**. Developed by **Novartis**, it was primarily investigated as an immunomodulatory agent for the prevention of transplant rejection and the treatment of autoimmune diseases. AUY954 works by binding to S1PR1 on the surface of lymphocytes, which triggers the internalization and subsequent degradation of the receptor. This process, known as functional antagonism, prevents lymphocytes from sensing the S1P gradient required for their egress from lymphoid organs into the circulation, thereby reducing inflammatory cell infiltration. While it reached early clinical development (Phase 1) for renal transplantation, it is now frequently utilized as a high-affinity pharmacological tool in preclinical research to study S1P signaling in vascular development, cardiac morphogenesis, and immune responses.

Other names

2-amino-2-[2-[2-chloro-4-[[3-phenyl-5-(propan-2-yl)-1,2-oxazol-4-yl]methoxy]phenyl]ethyl]propane-1,3-diol