BChE-IN-41
BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC50 =12 nM, Ki = 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ1-42.
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- Fòrmula: C23H26N2O2S
- Peso molecular:394.53
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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hAChE 22110 nM (IC50) |
BChE-IN-41 (Compound (R)-(−)-3) (5 μM, 48 h) exhibits neuroprotective activity by diminishing Aβ1−42-induce SH-SY5Y cells death[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cells, SH-SY5Y cells
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Concentration:1 μM, 5 μM, 10 μM, 20 μM, 50 μM, 100 μM
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Incubation Time:48 h
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Result:Had comparable cytotoxicity profiles in both HepG2 cells and SH-SY5Y cells.
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Cell Line:SH-SY5Y cells
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Concentration:2.5 μM, 5 μM
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Incubation Time:48 h
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Result:Reversed Aβ toxicity and reduced cell death at 5 μM; its effect was not significant at 2.5 μM.
BChE-IN-41 (1-10 mg/kg, i.p, sing dose) improves contextual memory deficits and recognition memory deficits in adult male CD-1 mice induced by scopolamine[1].
BChE-IN-41 (10 mg/kg, i.p, at the corresponding doses for 14 days) improves learning ability and cognitive function in ICR male mice induced by Aβ1-42 oligomers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female and male wild-type Balb/c mice (3 months)[1]
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Dosage:10 mg/kg, 100 mg/kg
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Administration:Oral gavage (i.g.), sing dose
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Result:Exhibited high brain penetration with a brain-to-plasma ratio of 9.0.
Caused no mortality or tissue lesions in mice, and no abnormalities were found in histological examination.
Caused steady weight gain with no signs of acute toxicity.
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Animal Model:Scopolamine (HY-N0296) (1 mg/kg, s.c) induced AD model in adult male CD-1 mice (18-22 g)[1]
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Dosage:1 mg/kg, 10 mg/kg
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Administration:Intraperitoneal injection (i.p.), sing dose
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Result:Prolonged the latency to enter the dark chamber and improved the contextual memory deficit.
Demonstrated prolonged step-through latency compared to mice treated with scopolamine only.
Enhanced preference for novel objects and increased the discrimination index (DI) and reversed the recognition memory deficit.
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Animal Model:Aβ1-42 oligomers (10 µg per mouse, i.c.v) induced AD-like cognitive deficits model in ICR male mice (8-10 weeks, 18−20 g)[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection (i.p.), at the corresponding doses for 14 days.
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Result:Caused no motor impairment in the rotarod test (6/18/24 rpm).
Resulted in shorter escape latency and shorter distance to reach the target area, and improved Aβ1-42-induced cognitive deficits.
Chemical Information
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Peso molecular 394.53
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Fòrmula C23H26N2O2S
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SMILES
CN(S(=O)(C1=CC=C(C=CC=C2)C2=C1)=O)C[C@@H](C3)CCN3CC4=CC=CC=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BChE-IN-41 Related Classifications
HY-174381 Related Classifications
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