ChemicalBook > CAS DataBase List > PE859

PE859

Product Name
PE859
CAS No.
1402727-29-0
Chemical Name
PE859
Synonyms
PE859;PE-859; PE 859;PE859, 10 mM in DMSO;AMBZHNVCLPHAKA-NSJFVGFPSA-N;PE 859,PE-859,Inhibitor,inhibit,Microtubule/Tubulin,PE859;1H-Indole, 6-[(1E)-2-[5-[(1E)-2-[2-methoxy-4-(2-pyridinylmethoxy)phenyl]ethenyl]-1H-pyrazol-3-yl]ethenyl]-
CBNumber
CB33161550
Molecular Formula
C28H24N4O2
Formula Weight
448.52
MOL File
1402727-29-0.mol
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PE859 Property

Boiling point:
747.7±60.0 °C(Predicted)
Density 
1.312±0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
DMSO : 50 mg/mL (111.48 mM);Water : < 0.1 mg/mL (insoluble)
form 
Solid
pka
13.78±0.10(Predicted)
color 
Light yellow to khaki
InChIKey
AMBZHNVCLPHAKA-NSJFVGFPSA-N
SMILES
N1C2=C(C=CC(/C=C/C3C=C(/C=C/C4=CC=C(OCC5=NC=CC=C5)C=C4OC)NN=3)=C2)C=C1
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

TRC
Product number
M267212
Product name
6-((E)-2-(3-((E)-2-Methoxy-4-(pyridin-2-ylmethoxy)styryl)-1H-pyrazol-5-yl)vinyl)-1H-indole
Packaging
2.5mg
Price
$800
Updated
2021/12/16
ChemScene
Product number
CS-6428
Product name
PE859
Purity
99.84%
Packaging
10mg
Price
$600
Updated
2021/12/16
ChemScene
Product number
CS-6428
Product name
PE859
Purity
99.84%
Packaging
1mg
Price
$132
Updated
2021/12/16
ChemScene
Product number
CS-6428
Product name
PE859
Purity
99.84%
Packaging
5mg
Price
$396
Updated
2021/12/16
ChemScene
Product number
CS-6428
Product name
PE859
Purity
99.84%
Packaging
50mg
Price
$1800
Updated
2021/12/16
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PE859 Chemical Properties,Usage,Production

Uses

6-((E)-2-(3-((E)-2-Methoxy-4-(pyridin-2-ylmethoxy)styryl)-1H-pyrazol-5-yl)vinyl)-1H-indole is a potent tau aggregation inhibitor that functions as a drug for Alzheimer’s disease.

in vivo

PE859 could cross the blood-brain barrier and that PE859 could be distributed into the tissues of the central nervous system. The maximum concentration of PE859 is 2.005 μg/mL in the blood at 3 h and 1.428 μg/g in the brain at 6 h. PE859 delays onset and progression of the motor dysfunction in JNPL3 mice. PE859 delays progression of the motor dysfunction through the inhibition of accumulation of sarkosyl-insoluble tau. [2]

Enzyme inhibitor

This orally bioavailable tau aggregation inhibitor (FW = 448.53 g/mol; IUPAC: 3-[(1E)-2-(1H-indol-6-yl)ethenyl]-5-[(1E)-2-[2-methoxy-4-(2- pyridylmethoxy)phenyl]ethenyl]-1H-pyrazole) significantly reduces formation of sarkosyl-insoluble aggregates of Tau, the principal axonal microtubule-associated protein, and prevents onset and progression of the motor dysfunction in JNPL3 Pro-301-Leu-mutated human tau transgenic mice. PE859 also inhibits aggregation of three-repeat Tau, or 3RMBD-Tau (IC50 = 0.81 μM), and four-repeat Tau, or 2N4R-Tau (IC50 = 2.23 μM).

PE859 Preparation Products And Raw materials

Raw materials

Preparation Products

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1402727-29-0, PE859Related Search:


  • PE859
  • AMBZHNVCLPHAKA-NSJFVGFPSA-N
  • PE-859; PE 859
  • 1H-Indole, 6-[(1E)-2-[5-[(1E)-2-[2-methoxy-4-(2-pyridinylmethoxy)phenyl]ethenyl]-1H-pyrazol-3-yl]ethenyl]-
  • PE 859,PE-859,Inhibitor,inhibit,Microtubule/Tubulin,PE859
  • PE859, 10 mM in DMSO
  • 1402727-29-0