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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.01%
- CAS 番号: 1192750-33-6
- 分子式: C35H35N5O4
- 分子量:589.68
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保管条件:
-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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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hAChE 280 pM (IC50) |
hBCHE 16 nM (IC50) |
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.
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.
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化学情報
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CAS 番号 1192750-33-6
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性状 Solid
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分子量 589.68
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 |
|---|---|---|---|---|---|
| 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 関連分類
HY-103373 関連分類
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