AChE/BACE1/GSK3β-IN-1
AChE/BACE1/GSK3β-IN-1 is an orally active triple inhibitor of AChE/BACE1/GSK3β. AChE/BACE1/GSK3β-IN-1 has effective inhibitory activity against AChE, BACE1 and GSK3β with IC50 values of 1.0 μM, 20 μM and 15 μM, respectively. AChE/BACE1/GSK3β-IN-1 has good blood-brain barrier penetrability, suitable bioavailability. AChE/BACE1/GSK3β-IN-1 can be used for the research of Alzheimer's disease (AD).
For research use only. We do not sell to patients.
- CAS No.: 2866066-81-9
- Formula: C26H27FN2O4
- Molecular Weight:450.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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BACE1 20 μM (IC50) |
AChE 1 μM (IC50) |
GSK-3β 15 μM (IC50) |
AChE/BACE1/GSK3β-IN-1 (p.o., 100 mg/kg; i.v., 10 mg/kg)has good PK profiles[1].
AChE/BACE1/GSK3β-IN-1 (gavage, 2.5 mg/kg, 5 mg/kg and 10mg/kg, for 7 consecutive days) can ameliorate the impaired learning and memory in Aβ-induced AD mice[1].
AChE/BACE1/GSK3β-IN-1 inhibits the expression of ADAM17 in the cortex and significantly decreases the expressions of ADAM17 and BACE1 in AD mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57B6/J Mice[1]
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Dosage:200 and 400 mg/kg
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Administration:oral, single
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Result:Increased slightly serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST), but no significant difference.
Showed no significant change in the content of blood urea nitrogen (BUN).
Did not change significantly the morphology of liver and kidney tissue of mice.
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Animal Model:male Sprague-Dawley (SD) rats[1]
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Dosage:10 mg/kg and 100 mg/kg
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Administration:oral and intravenous
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Result:
parameters 100 mg/kg (p.o.) 10 mg/kg(i.v.) Cmax(ng/mL) 167 ± 13 2796 ± 259 AUC0−t(ng/mL) 1010 ± 112 1031 ± 86 AUC0−∞(ng/mL*h) 1635 ± 362 1047 ± 88 t1/2 (h) 20 ± 9 0.4 ± 0.04 Cl (L/h/kg) 63 ± 12 10 ± 1 MRT0−∞(h) 26 ± 11 0.3 ± 0 VZ(L/kg) 1730 ± 387 5 ± 1 Tmax(h) 1 0.08 F (%) 9.8
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Animal Model:Aβ-induced AD mice[1]
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Dosage:2.5 mg/kg, 5 mg/kg and 10mg/kg
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Administration:gavage, for 7 consecutive days
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Result:Decreased the escape latency of mice.
Increased the number of crossing platforms in mice in a dose-dependent trend.
Chemical Information
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CAS No. 2866066-81-9
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Molecular Weight 450.50
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Formula C26H27FN2O4
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SMILES
O=C1C=CC2=C(OCCCN3CCC(NCC4=CC(F)=CC=C4)CC3)C5=C(OC=C5)C=C2O1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE/BACE1/GSK3β-IN-1 Related Classifications
HY-151260 Related Classifications
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