PE154 free base · Synonyms: PE-154 · PE 154
PE154 is a potent fluorescent inhibitor of human acetylcholinesterase.
For research use only. Not for human or veterinary use.
PE154 structure
CAS No.: 1192750-33-6
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 480.00 | BP-02157-50mg | In stock | Get quote |
| 100 mg | USD 750.00 | BP-02157-100mg | In stock | Get quote |
| 250 mg | USD 1,500.00 | BP-02157-200mg | In stock | Get quote |
| 500 mg | USD 2,350.00 | BP-02157-500mg | In stock | Get quote |
| 1 g | USD 3,780.00 | BP-02157-1g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
PE154 (Compound 13) is a potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50s=280 pM and 16 nM, respectively). PE154 can label β-amyloid plaques in histochemical analysis.
Biological activity
n 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. 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. 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. In Vivo PE154 (2 μL (0.1 mg/mL); stereotaxic injection into dorsal hippocampus; single dose) selectively targets hippocampal β-amyloid plaques in aged triple-transgenic Alzheimer's disease model mice in vivo, with approximately 80% of rostral hippocampal Aβ plaques labelled as early as 4 hours post-intrahippocampal injection and labelling persisting for up to 7 days.
Identifiers
- SMILES
-
CCN(CC)C1=CC2=C(C=C1)C(=C(C(=O)O2)C=NC3=CC=C(C=C3)CC(=O)NNC4=C5CCCCC5=NC6=CC=CC=C64)O - InChIKey
-
RSKDYQUBLFFWPM-UHFFFAOYSA-N
Specifications
- MW (average)
- 589.6835
- Formula
- C35H35N5O4
- CAS No.
- 1192750-33-6
- Physical state
- Solid
- Color
- Light yellow to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; protect from light
Solubility
Soluble in DMSO : 8.33 mg/mL