hAChE/hBACE-1-IN-2
hAChE/hBACE-1-IN-2 is a potent, orally active, blood-brain barrier transboundary triple inhibitor of hAChE, hBChE, and HACE-1 with IC50s of 0.113 μM, 1.48 μM and 0.38 μM, respectively. hAChE/hBACE-1-IN-2 has antioxidant activity. hAChE/hBACE-1-IN-2 also inhibits Aβ11-42 aggregation. hAChE/hBACE-1-IN-2 can be used to study Alzheimer's disease.
For research use only. We do not sell to patients.
- Formula: C22H24N4O2S
- Molecular Weight:408.52
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hAChE 0.113 μM (IC50) |
hBACE-1 0.38 μM (IC50) |
hBCHE 1.48 μM (IC50) |
hAChE/hBACE-1-IN-2 (compound 5f) (10-80 μM; 72 h) is considered similar to Donepezil (HY-14566) in terms of safety in SH-SY5Y neuroblastoma cell lines[1].
hAChE/hBACE-1-IN-2 (compound 5f) (20 μM; 48 h, 72 h) has the potential of anti-Aβ1-42 aggregation potential in SH-SY5Y neuroblastoma cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cell lines (The SH-SY5Y cells were sequentially treated with RA and BDNF for 6 days)
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Concentration:10, 20, 40, and 80 μM
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Incubation Time:48-72 h
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Result:Indicated a similar reduction in the differentiated neuroblastoma cell population at a maximum 80 μM concentration.
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Cell Line:Aβ1-42 treated SH-SY5Y cells (incubated with Aβ1-42 (10μM) for 24 h)
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Concentration:20 μM
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Incubation Time:48-72 h
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Result:The cells incubated the cell viability to 65% and 75% after 48 h and 72 h.
hAChE/hBACE-1-IN-2 (500 mg/kg, p.o., 14 days) is well tolerated and has no apparent toxicity in Swiss albino mice, including brain, liver, kidneys, and heart abnormalities[1].
hAChE/hBACE-1-IN-2 (10 mg/kg, p.o., 14 days) crosses the blood-brain barrier, reduces AchE levels or substrate hydrolysis in hippocampal and cortical brain homogenates, delays oxidative stress and reduces the potential for pro-inflammatory cytokine levels in a mouse model induced by Scopolamine (HY-N0296)[1].
hAChE/hBACE-1-IN-2 (10 mg/kg, p.o., 14 days) inhibits BACE-1, Aβ, APP/Aβ, and tau protein, protect brain tissue in different brain regions in the Aβ-induced model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss albino mice[1]
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Dosage:500 mg/kg
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Administration:Oral administration (p.o.), 14 days
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Result:Showed no signs or symptoms of toxicity over the 14 days
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Animal Model:Scopolamine-induced cognitive deficit mouse model[1]
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Dosage:2.5 mg, 5 mg, and 10 mg/kg
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Administration:Oral administration (p.o.), 14 days
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Result:Elevated plus maze test showed significant reductions in transfer latency and time spent in open arms, similar to the effects observed with Scopolamine (HY-N0296)-induced dementia reversal.
Chemical Information
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Molecular Weight 408.52
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Formula C22H24N4O2S
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SMILES
O=C(CSC1=NN=C(C2=CC=CC=C2)O1)NC3CCN(CC3)CC4=CC=CC=C4
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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)
hAChE/hBACE-1-IN-2 Related Classifications
HY-149288 Related Classifications
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