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Cat. No.: HY-189724

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mtCI Modulator 1

mtCI Modulator 1 is an orally active and blood-brain barrier-permeable mtCI modulator. mtCI Modulator 1 reduces NADH oxidation/respiration, triggers adaptive stress signaling, activates AMPK to produce neuroprotective/antioxidant/autophagy/anti-inflammatory/mitochondrial biogenesis effects, and promotes Akt/AMPK-dependent inhibitory phosphorylation of GSK3β while reducing Tau phosphorylation. mtCI Modulator 1 prevents Aβ toxicity, increases oxidative stress resistance and NADPH/glutathione, inhibits NF-κB, induces autophagy/mitochondrial biogenesis, reduces Aβ/p-Tau in brain organoids, and improves mitochondrial reserve respiratory capacity. mtCI Modulator 1 activates AMPK-centered brain signaling in wild-type mice. mtCI Modulator 1 can be used for research on Alzheimer's disease.

For research use only. We do not sell to patients.

Formula: C₂₁H₃₂Cl₃N₃O₂
Molecular Weight:464.86

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Please store the product under the recommended conditions in the Certificate of Analysis.

mtCI Modulator 1 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All AMPK Isoforms :

All Akt Isoforms :

All GSK-3 Isoforms :

All NF-κB Isoforms :

In Vitro

Aβ/Tau/α-Synuclein AggregationMitochondrial FunctionCarbohydrate MetabolismOxidative StressInnate ImmunityCytokines & Chemokines

Aβ/Tau/α-Synuclein Aggregation

mtCI Modulator 1 (C273) (2 nM-5 μM for protective effects; 2 nM-100 μM for cytotoxicity) protects MC65 Tet-Off cells against Aβ-induced toxicity with an EC₅₀ of 14.2 nM and shows extremely low intrinsic cytotoxicity in MC65 Tet-On cells^[1].
mtCI Modulator 1 (48 h) reduces Aβ42/Aβ40 and p-Tau/Tau ratios in APOE4/4 late-onset AD brain organoids and activates AMPK/GSK3β signaling^[1].

Mitochondrial Function

Carbohydrate Metabolism

mtCI Modulator 1 (24 h for NADH detection; 1 h for OCR/ECAR detection) increases NADH levels in MC65 Tet-On cells and moderately decreases basal OCR without inducing compensatory glycolysis^[1].

Mitochondrial Function

mtCI Modulator 1 (2 nM-5 μM) protection in MC65 Tet-Off cells is blocked by pre-exposure to Rotenone (HY-B1756) (32 nM; 30 min), supporting a competitive interaction at the mtCI Q site^[1].
mtCI Modulator 1 improves mitochondrial bioenergetic adaptability in SH-SY5Y APPswe cells by increasing spare respiratory capacity^[1].

Oxidative Stress

Mitochondrial Function

mtCI Modulator 1 activates AMPK-dependent mitochondrial biogenesis, antioxidant defense, and anti-inflammatory signaling in WT MEFs, and these responses require AMPKα1/α2^[1].
mtCI Modulator 1 restores mitochondrial quality control and antioxidant protein expression in MC65 Tet-Off cells^[1].
mtCI Modulator 1 (1 μM) activates AMPK and downstream mitochondrial/antioxidant signaling in human PBMCs^[1].

Oxidative Stress

mtCI Modulator 1 (250 nM; 24 h) increases the resistance of MC65 Tet-Off cells to H₂O₂-induced toxicity and elevates NADPH and GSH levels^[1].

Innate Immunity

Cytokines & Chemokines

mtCI Modulator 1 inhibits NF-κB-dependent inflammatory signaling in stimulated HEK293 reporter cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_max (Plasma)	T_max (Brain)	C_max	AUC_last	AUC_inf	T_1/2 (Plasma)	T_1/2 (Brain)	MRT_last	F	C₀	CL	V_ss
Mice^[1]	3 mg/kg	i.v.	0.08 h	0.5 h	867 ng/mL	656 ng·h/mL	668 ng·h/mL	1.4 h	1.35 h	1.19 h	/	1121 ng/mL	74.9 mL/min/kg	5.33 L/kg
Mice^[1]	25 mg/kg	p.o.	0.25 h	0.5 h	3615 ng/mL	5844 ng·h/mL	5893 ng·h/mL	1.21 h	1.14 h	1.54 h	107 %	/	/	/

In Vivo

AutophagyMitochondrial Function

Autophagy

Mitochondrial Function

mtCI Modulator 1 (25 mg/kg; oral; single administration; up to 24 h) activates AMPK-centered brain signaling in wild-type mice, increasing markers of autophagy, survival, and mitochondrial biogenesis for up to 24 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C57BL/6J (male, 8-12 weeks old)^[1]
Dosage:

3 mg/kg; 25 mg/kg
Administration:

i.v., single dose; p.o., single dose
Result:

After a single p.o. dose of 25 mg/kg C273, brain tissue showed increased AMPKα phosphorylation within 30 min of oral administration.
Phosphorylation of ULK1 at Ser555 was increased, supporting autophagy induction.
Akt phosphorylation was increased, with corresponding inhibitory phosphorylation of GSK3β and FOXO3A.
Brain expression of PGC1α and Sirt3 was also increased, and these signaling effects persisted for up to 24 h after the single oral dose.

Related Protocols :

Chemical Information

Molecular Weight 464.86
Formula C₂₁H₃₂Cl₃N₃O₂
SMILES

CC1=CC=CC(OC2CCN(CC2)C[C@@H](NCC3=CC=[N+]([O-])C=C3)C)=C1.Cl.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Trushin S, et al. Discovery and preclinical validation of a translationally optimized mitochondrial complex I modulator for Alzheimer's disease. npj drug discovery. 2026 Sep 02;3(1):36.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

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100 mg

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Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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mtCI Modulator 1

All AMPK Isoforms

All Akt Isoforms

All GSK-3 Isoforms

All NF-κB Isoforms