PE154
Based on 1 Customer Validation
PE154 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 is applicable for histochemical detection of Aβ plaques in mouse and human brain tissues. PE154 can be used in research related to Alzheimer's disease.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.01%
- CAS. Nr.: 1192750-33-6
- Formel: C35H35N5O4
- Molecular Weight:589.68
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Speicherung:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-17387
(-)-Huperzine A -
HY-11017
Rivastigmine tartrate -
HY-103240
Methoxy-X04 -
HY-B1488
Tacrine hydrochloride -
HY-B0841
Acephate -
HY-103372
GSK264220A -
HY-N2320
Physostigmine hemisulfate -
HY-B0732
Itopride hydrochloride -
HY-103241
Ro 90-7501 -
HY-106901A
Asoxime dichloride -
HY-B0882
Edrophonium chloride -
HY-11017R
Rivastigmine tartrate (Standard)
Biologische Aktivität
Beschreibung
IC50 & Target
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hAChE 280 pM (IC50) |
hBCHE 16 nM (IC50) |
In Vitro
PE154 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 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 (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.
Emission (Em)
512
Chemical Information
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CAS. Nr. 1192750-33-6
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Appearance Solid
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Molecular Weight 589.68
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Formel C35H35N5O4
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Color Light yellow to yellow
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SMILES
O=C(NNC1=C(CCCC2)C2=NC3=CC=CC=C31)CC4=CC=C(N/C=C(C(C5=CC=C(N(CC)CC)C=C5O6)=O)/C6=O)C=C4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 8.33 mg/mL (14.13 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (285 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.6958 mL | 8.4792 mL | 16.9584 mL | 42.3959 mL |
| 5 mM | 0.3392 mL | 1.6958 mL | 3.3917 mL | 8.4792 mL | |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6958 mL | 4.2396 mL |
PE154 Related Classifications
HY-103373 Related Classifications
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