PE154 (solution)
PE154 (solution) is a fluorescent probe that binds to Aβ plaques, as well as a potent fluorescent inhibitor of AChE and BChE, with an IC50 of 280 pM against hAChE and 16 nM against hBChE. PE154 (solution) is applicable for histochemical detection of Aβ plaques in mouse and human brain tissues. PE154 (solution) can be used in research related to Alzheimer's disease.
Solvent and concentration: DMSO: 5 mM
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- CAS No.: 1192750-33-6
- Formule: C35H35N5O4
- Masse moléculaire:589.68
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Solvent and concentration: DMSO: 5 mM
IC50 & Target
[1]|
hAChE 280 pM (IC50) |
hBCHE 16 nM (IC50) |
In Vitro
PE154 (solution) reversibly binds to human acetylcholinesterase through active site cation-π stacking and interactions with the peripheral anionic site; its binding to human butyrylcholinesterase relies on active site cation-π stacking, with reduced effects on the peripheral site[2][3].
PE154 (solution) binds to the β-sheet structure of Aβ plaques independently of cholinesterase binding, exhibits enhanced fluorescence upon binding to cholinesterase, and can target Aβ deposits in the hippocampus when delivered via nanoparticle carriers[2][3].
PE154 (solution) (20 nM; 300 s) causes a significant increase in fluorescence intensity upon binding to purified recombinant human acetylcholinesterase and human butyrylcholinesterase, but this phenomenon is not observed when it binds to bovine serum albumin[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Triple-transgenic (TTG) (13-19 months old, harboring mutant human APPswe, PS-1, and tauP301L)[2]
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Dosage:2 μL (0.1 mg/mL)
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Administration:stereotaxic injection into dorsal hippocampus; single dose
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Result:Fluorescently labelled Aβ-immunopositive senile plaques in the hippocampus as early as 4 hours post-injection, with labelling persisting for up to 7 days.
Labelled approximately 80% of Aβ-immunoreactive plaques in rostral hippocampal regions (including the subiculum) in both hemispheres.
Primarily targeted the core of Aβ plaques, not the outer rim.
Selectively bound Aβ and did not target hyperphosphorylated tau or reactive astrocytes surrounding plaques.
Chemical Information
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CAS No. 1192750-33-6
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Masse moléculaire 589.68
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Formule C35H35N5O4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Brambilla D, et al. Nanotechnologies for Alzheimer's disease: diagnosis, therapy, and safety issues. Nanomedicine : nanotechnology, biology, and medicine. 2011 Oct;7(5):521-40. [Content Brief]
[2]. Härtig W, et al. In vivo labelling of hippocampal beta-amyloid in triple-transgenic mice with a fluorescent acetylcholinesterase inhibitor released from nanoparticles. The European journal of neuroscience. 2010 Jan;31(1):99-109. [Content Brief]
[3]. Elsinghorst PW, et al. A gorge-spanning, high-affinity cholinesterase inhibitor to explore beta-amyloid plaques. Organic & biomolecular chemistry. 2009 Oct 07;7(19):3940-6. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PE154 (solution) Related Classifications
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