| Identification | Back Directory | [Name]
PE859 | [CAS]
1402727-29-0 | [Synonyms]
PE859
PE-859; PE 859
AMBZHNVCLPHAKA-NSJFVGFPSA-N
1H-Indole, 6-[(1E)-2-[5-[(1E)-2-[2-methoxy-4-(2-pyridinylmethoxy)phenyl]ethenyl]-1H-pyrazol-3-yl]ethenyl]- | [Molecular Formula]
C28H24N4O2 | [MDL Number]
MFCD28411710 | [MOL File]
1402727-29-0.mol | [Molecular Weight]
448.52 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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. | [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). | [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] | [storage]
Store at -20°C |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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