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PE859
🥰Excellent
Catalog No. T4077Cas No. 1402727-29-0
PE859 is a potent inhibitor of the aggregation of both tau and Aβ.
PE859
🥰Excellent
Purity: 99.09%
Catalog No. T4077Cas No. 1402727-29-0
PE859 is a potent inhibitor of the aggregation of both tau and Aβ.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $61 | In Stock | |
| 5 mg | $147 | In Stock | |
| 10 mg | $228 | In Stock | |
| 25 mg | $428 | In Stock | |
| 50 mg | $683 | In Stock | |
| 100 mg | $1,060 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $162 | In Stock |
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Purity:99.09%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | PE859 is a potent inhibitor of the aggregation of both tau and Aβ. |
| Targets&IC50 | β-Amyloid:1.2 μM, Tau:0.66 μM |
| In vitro | In an Alzheimer's patient's brain, senile plaques and neurofibrillary tangles, the abnormal aggregates of amyloid β (Aβ) peptide and Tau Protein, are observed as the two major hallmarks of this disease. PE859 inhibits the heparin-induced aggregation of both 3RMBD and full length tau in a concentration-dependent manner. In each assay, the IC50 values calculated at the last measurement periods are 0.81 μM, and 2.23 μM, respectively. PE859 inhibits tau aggregation through the formation of a beta-sheet structure[2]. |
| In vivo | PE859 effectively crosses the blood-brain barrier, enabling its distribution within central nervous system tissues. It reaches a peak concentration of 2.005 μg/mL in blood at 3 hours and 1.428 μg/g in the brain by 6 hours. Notably, PE859 postpones the onset and advancement of motor dysfunction in JNPL3 mice by inhibiting the buildup of sarkosyl-insoluble tau. [2] |
| Kinase Assay | PEL cells are incubated in triplicate in a 96-well microculture plate in the presence of different concentrations of methyl-β-cyclodextrin (0-10 mM) in a final volume of 0.1 mL for 24 h at 37°C. Subsequently, MTT (0.5 mg/mL final concentration) is added to each well. After 3 h of additional incubation, 100 μL of a 0.04 N HCl is added to dissolve the crystals. Absorption values at 570 nm are determined. |
| Molecular Weight | 448.52 |
| Formula | C28H24N4O2 |
| Cas No. | 1402727-29-0 |
| Smiles | COc1cc(OCc2ccccn2)ccc1\C=C\c1cc(\C=C\c2ccc3cc[nH]c3c2)[nH]n1 |
| Relative Density. | 1.312 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 55 mg/mL (122.63 mM)  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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