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| Product Name: | PE859 | | Synonyms: | 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 | | CAS: | 1402727-29-0 | | MF: | C28H24N4O2 | | MW: | 448.52 | | EINECS: | | | Product Categories: | | | Mol File: | 1402727-29-0.mol |  |
| | PE859 Chemical Properties |
| 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) | | pka | 13.78±0.10(Predicted) |
| | PE859 Usage And Synthesis |
| 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). |
| | PE859 Preparation Products And Raw materials |
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