CYM-5442

CYM-5442 is a potent and highly selective small molecule agonist of the sphingosine 1-phosphate receptor 1 (S1P1), with an EC50 of approximately 1.35 nM. It exhibits significant selectivity for S1P1 over other receptor subtypes (S1P2-5), making it a valuable tool for studying S1P1-specific biological processes. The compound is orally bioavailable and brain-penetrant, with a plasma half-life of roughly 3 hours in rodent models. Preclinical research has demonstrated that CYM-5442 induces S1P1-dependent lymphopenia and activates downstream p42/p44 MAPK phosphorylation. While currently utilized primarily as a research tool, it has shown therapeutic potential in models of alcohol use disorder, acute graft-versus-host disease (aGVHD), neuropathic pain, and retinal ganglion cell protection. Notably, in alcohol dependence models, it has been shown to reduce consumption and motivation for alcohol with fewer aversive effects than some existing treatments.

Other names

2-(4-(5-(3,4-Diethoxyphenyl)-1,2,4-oxadiazol-3-yl)-2,3-dihydro-1H-inden-1-yl amino) ethanol hydrochloride