ILS-920

Names

[ Name ]:
ILS-920

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Research Areas >> Inflammation/Immunology

Research Areas >> Neurological Disease

[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].

[References]

[1]. Ruan B, et al. Binding of rapamycin analogs to calcium channels and FKBP52 contributes to their neuroprotective activities. Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):33-8.

Chemical & Physical Properties

[ Molecular Formula ]:
C₅₇H₈₆N₂O₁₄

[ Molecular Weight ]:
1023.30

Related Compounds

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