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PE859

PE859 is a potent inhibitor of the aggregation of both tau and Aβ.

Catalog No. T4077Cas No. 1402727-29-0

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Purity:99.09%

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COA LCMS HPLC HNMR

PE859

Catalog No. T4077Cas No. 1402727-29-0

PE859 is a potent inhibitor of the aggregation of both tau and Aβ.

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.

Pack Size	Price	Availability
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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Product Introduction

Bioactivity

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.

Chemical Properties

Molecular Weight	448.52
Formula	C₂₈H₂₄N₄O₂
Cas No.	1402727-29-0

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

	1mg	5mg	10mg	50mg
1 mM	2.2296 mL	11.1478 mL	22.2955 mL	111.4777 mL
5 mM	0.4459 mL	2.2296 mL	4.4591 mL	22.2955 mL
10 mM	0.2230 mL	1.1148 mL	2.2296 mL	11.1478 mL
20 mM	0.1115 mL	0.5574 mL	1.1148 mL	5.5739 mL
50 mM	0.0446 mL	0.2230 mL	0.4459 mL	2.2296 mL
100 mM	0.0223 mL	0.1115 mL	0.2230 mL	1.1148 mL

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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:

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

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 TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

Dose Conversion

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Tech Support

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