SR-31747

SR-31747 is a sigma ligand with immunosuppressive and anti-inflammatory properties. SR-31747 blocks cell proliferation by inhibiting sterol isomerase^[1][2]. IC50 & Target: Sigma ligand^[1] In Vitro: SR-31747 blocks the proliferation of lymphocytes at a concentration of 10 nM. SR-31747 is capable of inhibiting T-cell proliferation when added as late as 24 h after activation. SR-31747 arrests proliferation in yeast cells in a dose-dependent manner^[2]. In Vivo: In vivo, SR-31747 dramatically blocks lipopolysaccharide-induced production of IL-1, IL-6 and TNF-α in a dose-dependent manner (ED₅₀, 2 mg/kg). SR-31747 probably abrogated monokine production through an indirect mechanism that involves endogenous corticosteroids. This conclusion was supported by in vivo experiments that shows that: 1) ablation of corticosteroids by use of Mifepristone or adrenalectomy suppress the effect of SR-31747; 2) administration of SR-31747 induces an enhancement of the corticosterone level. SR-31747 improves the survival of animals with endotoxinic shock as a result of monokine inhibition^[1].