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.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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AChE 0.4 μM (IC50) |
AChE 0.28 μM (Ki) |
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.
| 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 |
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.
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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