ILS-920

ILS-920 is a nonimmunosuppressive Rapamycin analog with reduced immunosuppressive activity and potent neuroprotective activity. ILS-920 binds selectively to the immunophilin FKBP52 and to the β1-subunit of L-type voltage-gated calcium channels (VGCC). ILS-920 shows 200-fold selectivity for FKBP52 versus FKBP12^[1]. IC50 & Target: FKBP52^[1]
L-type voltage-gated calcium channels (VGCC)^[1] In Vitro: ILS-920 promotes neuronal survival and stimulates neurite outgrowth with potent neurotrophic activities in cortical neuronal cultures^[1].
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^[1]. In Vivo: In a transient middle cerebral artery occlusion (tMCAO) model of ischemic stroke, ILS-920, administered 4 h postocclusion at 10 and 30 mg/kg, significantly reduces infarct volume by 24% and 23% in 72 h, respectively, and robustly enhances functional recovery measured by improvement in neurological deficits^[1].