MAO-B-IN-45
MAO-B-IN-45 is a dual inhibitor of ferroptosis and MAO-B. MAO-B-IN-45 shows selectivity towards MAO-B with an IC50 of 87.47 nM and selectivity exceeding 229-fold for MAO-B over MAO-A. MAO-B-IN-45 has excellent antiferroptosis activity through modulation of the iron metabolic pathway and GSH-GPX4 axis in vitro. MAO-B-IN-45 improves cognitive and behavioral impairments in 3×Tg (APP/Tau/Ps1) AD mouse and significantly reduced the levels of ferritin heavy chain 1 (FTH1), APP, and Tau phosphorylation (p-Tau) proteins in the brain.
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- CAS No.: 3069915-36-9
- Formule: C17H14ClNO3
- Masse moléculaire:315.75
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Activité biologique
Description
IC50 & Target
[1]|
GPX4 |
hMAO-B 87.47 nM (IC50) |
In Vitro
MAO-B-IN-45 (compound 21d) is a reversible hMAO-B inhibitor with inhibition constant a Ki value of 100.6 nM , which displays high hMAO-B inhibitory activity, and the inhibition rate are 94.81% (10 μM) and 76.31% (1 μM)[1].
MAO-B-IN-45 (0.1-75 μM, 24 h) shows favorable safety in PC12 cells and HT22 cells[1].
MAO-B-IN-45 (1-50 μM, 24 h) effectively mitigates ferroptosis induced by RSL3 (HY-100218A) or Erastin (HY-15763) in a dose-dependent manner in HT22 cells[1].
MAO-B-IN-45 (10-50 μM, 24 h) reduces intracellular ROS production in HT22 cells[1].
MAO-B-IN-45 (15-100 μM, 24 h) effectively suppresses ferroptosis by both reducing intracellular iron accumulation and enhancing the GSH dependent pathway in HT22 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT22 cells, PC12 cells
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Concentration:25, 50, and 75 μM (HT22 cells), 0.1, 1, 10, 20, 30, 40, 50, 75 μM (PC12 cells)
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Incubation Time:24 h
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Result:Showed favorable safety, maintaining a cell viability of 83.56% on PC12 cells and 86.47% on HT22 cells at the highest test concentration (75 μM), warranting further investigation.
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Cell Line:RSL3/Erastin-induced HT22 cells
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Concentration:1, 5, 10, 25, 50 μM
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Incubation Time:24 h
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Result:Reduced ferroptosis induced by RSL3 and Erastin at a concentration of 10 μM and completely restored cell viability to normal levels at 50 μM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Triple-transgenic (APP/Tau/Ps1) mice (30-35 g, 7 months)[1].
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection daily for 35 days
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Result:Increased the number of entries, and reduced the latency and distance to the platform, showing effects comparable to those observed in the safinamide and donepezil groups.
Not markedly different from wild-type mice in cognitive function.
No abnormalities in the tissues (heart, liver, spleen, lung, kidney) compared to those of wild type mice (H&E staining).
Normalized FTH1 levels in 3×Tg mice, and significantly increased the expression level of GPX4.
Reduced the protein level of APP, and decreased the site-specificity in p-Tau at Ser202/Thr205.
Chemical Information
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CAS No. 3069915-36-9
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Masse moléculaire 315.75
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Formule C17H14ClNO3
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SMILES
CN1C(C(O)=CC2=CC=C(C=C21)OCC3=CC=C(C=C3)Cl)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MAO-B-IN-45 Related Classifications
HY-176271 Related Classifications
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