AChE/BChE-IN-35
AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC50 of 123.66 nM, human AChE IC50 of 122.34 nM, and equine BChE IC50 of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease.
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- Formule: C26H30N4O3
- Masse moléculaire:446.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
[1]|
hAChE 122.34 nM (IC50) |
electric eel AChE 123.66 nM (IC50) |
eqBCHE 488.00 nM (IC50) |
In Vitro
AChE/BChE-IN-35 (Compound L3) (5 min) inhibits eeAChE, hAChE, and eqBChE with IC50 values of 123.66 nM, 122.34 nM, and 488.00 nM, respectively[1].
AChE/BChE-IN-35 (50-100 μM; 24 h) shows low cytotoxicity toward bEnd.3 cells, with viability remaining close to 80% after 24 h treatment at 100 μM[1].
AChE/BChE-IN-35 (5 μg/mL; 30-300 min) crosses an in vitro bEnd.3 cell blood-brain barrier model with an apparent permeability coefficient of 11.25 × 10-6 cm/s[1].
AChE/BChE-IN-35 (4 h) is transported into U87 cells via LAT1, as shown by undetectable intracellular levels in the presence of an LAT1 competitive inhibitor[1].
AChE/BChE-IN-35 (10-50 μM; 24 h) shows low cytotoxicity toward HBMEC, BV2, PC-12, SH-SY5Y, with viability remaining above 50% at tested concentrations after 24 h treatment[1].
AChE/BChE-IN-35 (10-100 μM; 24 h) shows low hepatotoxicity in HepG2 and L02 cells, with viability remaining above 50% at tested concentrations after 24 h treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:mouse brain microvascular endothelial cells (bEnd.3)
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Concentration:50, 100 μM
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Incubation Time:24 h
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Result:Maintained cell viability close to 80% at 100 μM.
Maintained cell viability nearly 100% at 50 μM.
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Cell Line:human brain microvascular endothelial cells (HBMEC), murine microglial cells (BV2), rat adrenal pheochromocytoma cells (PC-12), human neuroblastoma cells (SH-SY5Y), human normal hepatocyte (L02), human hepatocellular carcinoma cells (HepG2)
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Concentration:10, 20, 50, 100 μM (HBMEC, BV2, PC-12, SH-SY5Y); 1.25, 2.5, 5, 10, 20, 50, 100, 200 μM (HepG2, L02)
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Incubation Time:24 h
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Result:Maintained viability above 50% across 10-50 μM in HBMEC, BV2, PC-12, and SH-SY5Y cells.
Maintained viability above 50% across 10-100 μM in HepG2 and L02 cells.
Parmacokinetics
| Species | Dose | Route | AUC | Brain-to-Plasma Ratio | Tmax |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 20037 min·ng/mL | 68 % | 15 min |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 446.54
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Formule C26H30N4O3
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SMILES
OC([C@H](N)CC1=CC(C(NCCCNC2=C3C(C=CC=C3)=NC4=C2CCCC4)=O)=CC=C1)=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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)