Chemical Structure : Mitochondrial complex I inhibitor C458
CAS No.:
2001090-87-3
Mitochondrial complex I inhibitor C458
(cis-C458 isomer)
Catalog No.: PC-24451Not For Human Use, Lab Use Only.
C458 is nontoxic mitochondrial complex I (mtCI) inhibitor with highly protective against Aβ toxicity, C458 protects MC65 Tet-Off cells (Aβ expressed) with an EC50 of 4.6 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
C458 is nontoxic mitochondrial complex I (mtCI) inhibitor with highly protective against Aβ toxicity, C458 protects MC65 Tet-Off cells (Aβ expressed) with an EC50 of 4.6 nM.
C458 does not cause cell death in WT mouse cortical neurons at <10 uM.
C458 (1 uM) reduces mtCI activity by ~15%.
C458 at nanomolar concentrations weakly inhibits mtCI, protecting MC65 cells from Aβ toxicity without causing cytotoxicity or inducing glycolysis.
C458 penetrates the BBB, directly interacts with mtCI, and activates neuroprotective pathways in the mouse brain.
C458 treatment (25 mg/kg/day, 0.05% DMSO) alleviates the AD-like phenotype in APP/PS1 mice, enhances metabolic flexibility and energy homeostasis in the brain and periphery.
C458 treatment requires AMPK activation, which induces multiple neuroprotective mechanisms in vivo and in vitro.
Physicochemical Properties
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M.Wt
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338.50
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Formula
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C22H30N2O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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cis-(N-(pyridin-4-ylmethyl)-2-(3-(m-tolyloxy)cyclohexyl)propan-1-amine
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References
1. Trushin S, et al. bioRxiv [Preprint]. 2025 Feb 17:2025.02.12.637918.
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