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mtCI modulator C273

Chemical Structure : mtCI modulator C273

CAS No.:

mtCI modulator C273

货号: PC-26649Not For Human Use, Lab Use Only.

mtCI modulator C273 is a selective, brain-penetrant, orally bioavailable small molecule modulator/ weak inhibitor of mitochondrial complex I (mtCI) with IC50 of 201.5 uM, protects against Aβ toxicity through mtCI modulation.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

mtCI modulator C273 is a selective, brain-penetrant, orally bioavailable small molecule modulator/ weak inhibitor of mitochondrial complex I (mtCI) with IC50 of 201.5 uM, protects against Aβ toxicity through mtCI modulation.
C273 protects MC65 Tet-Off cells from Aβ-induced toxicity with an EC50 of 14.2 nM, with no detectable cytotoxicity.
C273 is a selective, weak inhibitor (IC50=201.5 uM) of the mtCI quinone binding site, shows no detectable inhibition of complexes II, III, or IV, confirming selectivity for mtCI.
C273 engages the Q site of mtCI and that its weak inhibition of mtCI is required for protection against Aβ toxicity.
C273 activates AMPK-centered neuroprotective signaling in the brain, increases phosphorylation of AMPKα and phosphorylation of ULK1 at Ser555.
C273 activates AMPK-dependent mitochondrial stress signaling and neuroprotective pathways, mitigates oxidative stress and inflammatory signaling.
C273 activates target engagement biomarkers in PBMCs and reduce Aβ and pTau in human LOAD organoids, reduces Aβ and p-Tau levels in patient-derived LOAD cerebral organoids.

物理化学性质&存储条件

分子量 355.48
分子式 C21H29N3O2
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

(S)-4-(((1-(4-(m-tolyloxy)piperidin-1-yl)propan-2-yl)amino)methyl)pyridine 1-oxide

参考文献

1. Trushin S, et al. bioRxiv [Preprint]. 2026 Apr 14:2026.04.10.717554.

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