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.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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hAChE 122.34 nM (IC50) |
electric eel AChE 123.66 nM (IC50) |
eqBCHE 488.00 nM (IC50) |
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.
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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.
| Species | Dose | Route | AUC | Brain-to-Plasma Ratio | Tmax |
|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 20037 min·ng/mL | 68 % | 15 min |
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.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/BChE-IN-35 Related Classifications
HY-182254 Related Classifications
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