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
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
N-Bromosuccinimide Price
- 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
- Product number
- CS-6428
- Product name
- PE859
- Purity
- 99.84%
- Packaging
- 10mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- CS-6428
- Product name
- PE859
- Purity
- 99.84%
- Packaging
- 1mg
- Price
- $132
- Updated
- 2021/12/16
- Product number
- CS-6428
- Product name
- PE859
- Purity
- 99.84%
- Packaging
- 5mg
- Price
- $396
- Updated
- 2021/12/16
- Product number
- CS-6428
- Product name
- PE859
- Purity
- 99.84%
- Packaging
- 50mg
- Price
- $1800
- Updated
- 2021/12/16
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
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