AChE-IN-24

Cat. No.: HY-151152: FAQs
Data Sheet Handling Instructions

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AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC₅₀ value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD).

For research use only. We do not sell to patients.

AChE-IN-24 Chemical Structure

CAS No. : 3033542-32-1

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

AChE

In Vitro

AChE-IN-24 (compound 4c2) has good hAChE inhibitory activity with IC₅₀values of 0.053 μM but owns little inhibition to hBuChE^[1].
AChE-IN-2 has inhibitory activity for electric eel acetylcholinesterase (eeAChE) and equine serum butyrylcholinesterase (eqBuChE) with IC₅₀values of 0.088 μM and 7.5μM, respectively^[1].
AChE-IN-24 (0-0.2 μM) can cross the BBB comfortably by means of passive diffusion^[1].
AChE-IN-2 (0-40 μM) triggers the translocation of Nrf2 to the nucleus, thereby expediting the binding of Nrf2 to the ARE for the transcription process^[1].
AChE-IN-2 (7 μM) significantly induces the expression of antioxidant-related enzymes by activating Nrf2 in BV-2 cells^[1].
AChE-IN-2 (1, 3, 7 μM) protects cells from H2O2-induced damage and inhibits ROS accumulation^[1].
AChE-IN-2 (1, 3, 7 μM) attenuates inflammatory responses^[1].

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

Cell Viability Assay^[1]

Cell Line:	BV-2 microglial cells
Concentration:	0, 2.5, 5, 10, 20 and 40 μM
Incubation Time:	24 h
Result:	Not observed significant cytotoxicity.

Western Blot Analysis^[1]

Cell Line:	BV-2 microglial cells
Concentration:	7 μM
Incubation Time:	0-15 h
Result:	Up-regulated the amount of total Nrf2 in a time-dependent manner, decreased gradually the cytosolic Nrf2 level with its continuous accumulation in the nucleus and increased the total cellular Nrf2 accumulation in concentration-dependently. Increased the protein expression levels of HO-1, NQO1, and GPX4 in a concentration-dependent manner with the biggest upregulation observed at 10 μM and significantly increased the protein levels of HO-1, NQO1, and GPX4 reaching the maximum at 9h, 6 h, and 3 h, respectively^[1].

In Vivo

AChE-IN-24 (compound 4c2) (oral; 0, 625, 1250, and 2500 mg/kg) is well tolerated and no toxicity in KM mice^[1].
AChE-IN-24 (7.5 mg/kg, 15 mg/kg and 30mg/kg; once) ameliorates cognitive deficit induced by Scopolamine, suggesting a practicable therapeutic effect on AD^[1].

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

Animal Model:	KM mice^[1]
Dosage:	0, 625, 1250, and 2500 mg/kg
Administration:	oral; 0, 625, 1250, and 2500 mg/kg
Result:	Not discovered abnormal behavior and acute toxicity were monitored for the first 4 h after administration, no acute neurological toxicities inclusive of tremor, convulsion, and death and no obvious signs of poisoning in the heart, liver, lungs, kidneys, and brain.

Animal Model:	The cognitive deficit mice model^[1]
Dosage:	7.5 mg/kg, 15 mg/kg and 30mg/kg
Administration:	7.5 mg/kg, 15 mg/kg and 30mg/kg; once
Result:	Reversed the step-down latency and number of errors in a concentration-dependent manner.

Molecular Weight

450.61

Formula

C₂₂H₃₀N₂O₄S₂

CAS No.

3033542-32-1

SMILES

O=C(OC)/C=C/C(NC1=CC=CC(OCCCCSC(N2C(C)CCCC2)=S)=C1)=O

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

Handling Instructions (2659 KB)

References

[1]. Jie Guo, et al. A multi-target directed ligands strategy for the treatment of Alzheimer's disease: Dimethyl fumarate plus Tranilast modified Dithiocarbate as AChE inhibitor and Nrf2 activator. Eur J Med Chem. 2022 Aug 11;242:114630. [Content Brief]

AChE-IN-24 Related Classifications

Neurological Disease

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Help & FAQs

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:

AChE-IN-243033542-32-1Cholinesterase (ChE)AChEBBBhAChEAlzheimer s disease (AD)neurosurgeryInhibitorinhibitorinhibit

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