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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C21H32Cl3N3O2
- 分子量:464.86
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
AMPK アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
体外実験
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].
mtCI Modulator 1 improves mitochondrial bioenergetic adaptability in SH-SY5Y APPswe cells by increasing spare respiratory capacity[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Tmax (Plasma) | Tmax (Brain) | Cmax | AUClast | AUCinf | T1/2 (Plasma) | T1/2 (Brain) | MRTlast | F | C0 | CL | Vss |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 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 % | / | / | / |
体内実験
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.
- Kinase activity and phosphorylation assays
- Western Blot
- ROS/oxidative-stress fluorescent staining
- Autophagy
- Lysosome and acidic-vesicle live-cell staining
- Research Protocol for Inflammation-related Diseases
- Protocol for Kinase activity and phosphorylation assays
- Cerebral Organoid Culture
- Macroautophagy Solutions
- Alzheimer’s Disease Modeling
化学情報
-
分子量 464.86
-
分子式 C21H32Cl3N3O2
-
SMILES
CC1=CC=CC(OC2CCN(CC2)C[C@@H](NCC3=CC=[N+]([O-])C=C3)C)=C1.Cl.Cl.Cl
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
mtCI Modulator 1 関連分類
HY-189724 関連分類
Powered by Bioz
Keywords
- mtCI Modulator 1
- mtCI Modulator1
- mtCI Modulator-1
- AMPK
- Autophagy
- Akt
- GSK-3
- Tau Protein
- Amyloid-β
- NF-κB
- APOE4
- Alzheimer's disease
- Aβ toxicity
- CYP
- GSK3β
- H2O2
- MEFs
- NADH oxidation
- NADPH
- PBMCs
- SH-SY5Y
- Tau phosphorylation
- anti-inflammatory
- antioxidant
- autophagy
- blood-brain barrier
- brain-to-plasma distribution
- cerebral organoids
- electron transport chain
- glutathione
- glycolysis
- hERG
- metformin
- mitochondrial biogenesis
- mitochondrial quality control
- mitochondrial spare respiratory capacity
- mtCI
- neuroprotective
- oxidative stress
- quinone site
- respiration
- rotenone
- Inhibitor
- inhibitor
- inhibit