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Mitochondrial complex I inhibitor C458

Chemical Structure : Mitochondrial complex I inhibitor C458

CAS No.: 2001090-87-3

Mitochondrial complex I inhibitor C458 (cis-C458 isomer)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 338.50
分子式 C22H30N2O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

cis-(N-(pyridin-4-ylmethyl)-2-(3-(m-tolyloxy)cyclohexyl)propan-1-amine

参考文献

1. Trushin S, et al. bioRxiv [Preprint]. 2025 Feb 17:2025.02.12.637918.

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