AChE-IN-94
AChE-IN-94 is an orally active and blood-brain barrier penetrable AChE inhibitor with an IC50 of 0.40 μM and Ki of 0.28 μM. AChE-IN-94 prevents self-induced and AChE-mediated Aβ1-42 aggregation. AChE-IN-94 alleviates cognitive/memory deficits in Scopolamine (HY-N0296)-induced amnesic model. AChE-IN-94 can be used for the study of Alzheimer's disease (AD).
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- 화학식: C20H18ClFN4O2S
- 분자량:432.90
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보관:
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
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
AChE 0.4 μM (IC50) |
AChE 0.28 μM (Ki) |
In Vitro
AChE-IN-94 (Compound LB05) exhibits potent inhibitory activity against AChE with an IC50 of 0.40 μM and an inhibition constant (Ki) of 0.28 μM[1].
AChE-IN-94 (10-50 μM) displaces propidium iodide (PI) from the peripheral anionic site (PAS) of AChE in a dose-dependent manner[1].
AChE-IN-94 (5-20 μM, 48 h incubation, in vitro) inhibits Aβ₁₋₄₂ aggregation in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Cmax | Tmax | AUC | T1/2 | CL/F | Vd/F | MRT |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.g. | 6.76 μg/mL | 2 h | 39.34 μg·h/mL | 6.11 h | 190 mL/h/kg | 1540 mL/kg | 9.65 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scopolamine-induced amnesia rat model: Male Wistar rats (160-180 g) were injected with scopolamine (3 mg/kg, i.p.) on the 7th day[1]
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Dosage:5, 10, 20 mg/kg
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Administration:p.o., once daily for 7 days
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Result:Ameliorated cognitive deficits in a dose-dependent manner.
Restored the percentage of spontaneous alternation (reflecting spatial working memory) and the total number of arm entries (reflecting exploratory activity).
Improved cholinergic function and reduced oxidative stress in the hippocampus.
Decreased AChE activity, reduced malondialdehyde (MDA) levels, and elevated catalase (CAT) activity.
Chemical Information
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분자량 432.90
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화학식 C20H18ClFN4O2S
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SMILES
O=C(NC1=NC2=CC=C(Cl)C=C2S1)CN3CCN(C(C4=CC=C(F)C=C4)=O)CC3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocol
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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.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AChE-IN-94 Related Classifications
HY-175758 Related Classifications
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