PE 154Fluorescent, potent AChE and BChE inhibitor CAS# 1192750-33-6 |
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Quality Control & MSDS
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| Cas No. | 1192750-33-6 | SDF | Download SDF |
| PubChem ID | 118797246 | Appearance | Powder |
| Formula | C35H35N5O4 | M.Wt | 589.68 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 50 mM in DMSO | ||
| Chemical Name | 2-[4-[[7-(diethylamino)-2,4-dioxochromen-3-ylidene]methylamino]phenyl]-N'-(1,2,3,4-tetrahydroacridin-9-yl)acetohydrazide | ||
| SMILES | CCN(CC)C1=CC2=C(C=C1)C(=O)C(=CNC3=CC=C(C=C3)CC(=O)NNC4=C5CCCCC5=NC6=CC=CC=C64)C(=O)O2 | ||
| Standard InChIKey | CYZIIGRHLSZNAV-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C35H35N5O4/c1-3-40(4-2)24-17-18-27-31(20-24)44-35(43)28(34(27)42)21-36-23-15-13-22(14-16-23)19-32(41)38-39-33-25-9-5-7-11-29(25)37-30-12-8-6-10-26(30)33/h5,7,9,11,13-18,20-21,36H,3-4,6,8,10,12,19H2,1-2H3,(H,37,39)(H,38,41) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent fluorescent inhibitor of human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) (IC50 values are 280 pM and 16 nM respectively). Targets and labels β-amyloid plaques in histochemical analysis. |
PE 154 Dilution Calculator
PE 154 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.6958 mL | 8.4792 mL | 16.9584 mL | 33.9167 mL | 42.3959 mL |
| 5 mM | 0.3392 mL | 1.6958 mL | 3.3917 mL | 6.7833 mL | 8.4792 mL |
| 10 mM | 0.1696 mL | 0.8479 mL | 1.6958 mL | 3.3917 mL | 4.2396 mL |
| 50 mM | 0.0339 mL | 0.1696 mL | 0.3392 mL | 0.6783 mL | 0.8479 mL |
| 100 mM | 0.017 mL | 0.0848 mL | 0.1696 mL | 0.3392 mL | 0.424 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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In vivo labelling of hippocampal beta-amyloid in triple-transgenic mice with a fluorescent acetylcholinesterase inhibitor released from nanoparticles.[Pubmed:20092557]
Eur J Neurosci. 2010 Jan;31(1):99-109.
The drastic loss of cholinergic projection neurons in the basal forebrain is a hallmark of Alzheimer's disease (AD), and drugs most frequently applied for the treatment of dementia include inhibitors of the acetylcholine-degrading enzyme acetylcholinesterase (AChE). This protein is known to act as a ligand of beta-amyloid (Abeta) in senile plaques, a further neuropathological sign of AD. Recently, we have shown that the fluorescent, heterodimeric AChE inhibitor PE154 allows for the histochemical staining of cortical Abeta plaques in triple-transgenic (TTG) mice with age-dependent beta-amyloidosis and tau hyperphosphorylation, an established animal model for aspects of AD. In the present study, we have primarily demonstrated the targeting of Abeta-immunopositive plaques with PE154 in vivo for 4 h up to 1 week after injection into the hippocampi of 13-20-month-old TTG mice. Numerous plaques, double-stained for PE154 and Abeta-immunoreactivity, were revealed by confocal laser-scanning microscopy. Additionally, PE154 targeted hippocampal Abeta deposits in aged TTG mice after injection of carboxylated polyglycidylmethacrylate nanoparticles delivering the fluorescent marker in vivo. Furthermore, biodegradable core-shell polystyrene/polybutylcyanoacrylate nanoparticles were found to be suitable, alternative vehicles for PE154 as a useful in vivo label of Abeta. Moreover, we were able to demonstrate that PE154 targeted Abeta, but neither phospho-tau nor reactive astrocytes surrounding the plaques. In conclusion, nanoparticles appear as versatile carriers of AChE inhibitors and other promising drugs for the treatment of AD.
A gorge-spanning, high-affinity cholinesterase inhibitor to explore beta-amyloid plaques.[Pubmed:19763296]
Org Biomol Chem. 2009 Oct 7;7(19):3940-6.
Cholinesterases are involved in the pathological formation of beta-amyloid plaques. To investigate this pathohistological hallmark of Alzheimer's disease we prepared a high-affinity, fluorescent cholinesterase inhibitor. Its fluorescence intensity was significantly enhanced upon binding to cholinesterases. Using this probe, brain samples from mice and humans affected by Alzheimer's disease were successfully analyzed for beta-amyloid plaques. Unexpectedly, it was discovered, by competition experiments, that the compound binds to amyloid structures, rather than to cholinesterases inside of the plaques.
