2. Neuronal Signaling
  3. Cholinesterase (ChE) Amyloid-β
  4. hAChE/hBACE-1-IN-4

hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research.

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hAChE/hBACE-1-IN-4 Chemical Structure

hAChE/hBACE-1-IN-4 Chemical Structure

CAS No. : 229476-71-5

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hAChE/hBACE-1-IN-4 Related Antibodies

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Description

hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research[1].

IC50 & Target[1]

hAChE

0.283 μM (IC50)

hBCHE

0.231 μM (IC50)

In Vitro

hAChE/hBACE-1-IN-4 (10, 20, 40 and 80 μM; 24 h) has non-neurotoxic properties[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

hAChE/hBACE-1-IN-4 Related Antibodies

Cell Viability Assay[1]

Cell Line: SH-SY5Y
Concentration: 10, 20, 40 and 80 μM
Incubation Time: 24 h
Result: Reduced cell viability by 26% at maximum concentration (80 μM).
In Vivo

hAChE/hBACE-1-IN-4 (500 mg/kg; po, 14 days) possesses a substantial margin of safety and is safe to be utilized for further in-vivo investigations in Wistar rats[1].
hAChE/hBACE-1-IN-4 (20 mg/kg; po, 9 days) inhibits ACE-1 activity to restore cognitive deficits and acts as an anti-Aβ agent at its tested doses in Wistar rats[1].
hAChE/hBACE-1-IN-4 (10 and 20 mg/kg; ig, 4 days) possesses the ability to cross the BBB and reaches their specific site of action in the brain[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar rats [1]
Dosage: 500 mg/kg for 14 days
Administration: Oral gavage (p.o.)
Result: Observed the renal and hepatic functional parameters within the prescribed limits
. Examined and found with normal tissue appearance such as kidneys, heart, liver, and brains.
Animal Model: Wistar rats [1]
Dosage: 20mg/kg for 9 days
Administration: Oral gavage (p.o.)
Result: Decreased the ELT and increased total platform crossing as compared to the diseased model group
. Increased the neuronal density and neuronal arrangement.
Animal Model: Wistar rats[1]
Dosage: 10 and 20 mg/kg for 4 days
Administration: i.g.
Result: The concentrations of AK-2 in brain homogenates were observed to 0.633 and 0.977 μg/mL.
Molecular Weight

364.44

Formula

C21H24N4O2
CAS No.
SMILES

COC1=C(OC)C=C2C(N(CC3)CCN3CC4=CC=CC=C4)=NC=NC2=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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hAChE/hBACE-1-IN-4 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

hAChE/hBACE-1-IN-4229476-71-5Cholinesterase (ChE)Amyloid-ββ-amyloid peptideAβAbetahAChE/hBACE InhibitorAlzheimer’s diseaseWistar ratsInhibitorinhibitorinhibit

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