ILS-920 is a Rapamycin analog characterized by diminished immunosuppressive effects but remarkable neuroprotective properties. It exhibits selective binding affinity towards the immunophilin FKBP52 as well as the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 displays a notable 200-fold preference for FKBP52 over FKBP12.

ILS-920 can inhibit L-type Ca2+ channels in rat hippocampal neurons and F-11 dorsal root ganglia (DRG)/neuroblastoma cells. ILS-920 can protect neurons from Ca2+-induced cell death by modulating Ca2+ channels and promote neurite outgrowth via FKBP52 binding.ILS-920 promotes neuronal survival and stimulates neurite outgrowth with potent neurotrophic activities in cortical neuronal cultures.

In a transient middle cerebral artery occlusion (tMCAO) model of ischemic stroke, administration of ILS-920 at 4 hours post-occlusion at dosages of 10 and 30 mg/kg significantly reduced infarct volume by 24% and 23% within 72 hours, respectively, and markedly improved functional recovery, as evidenced by the amelioration of neurological deficits.