- Shanghai Nianxing Industrial Co., Ltd
- China
- Product Name: PE859
- Price:
- Purity: 98.0%
- Stocking Period: Inquiry
- Contact: Tom
- DC Chemicals Limited
- China
- Product Name: PE859
- Price: $650.0/100mg $1200.0/250mg $2500.0/1g
- Purity: 98.0%
- Stocking Period: 3 Day
- Contact: Tony Cao
1402727-29-0
1402727-29-0 structure
- Name: PE859
- Chemical Name: PE859
- CAS Number: 1402727-29-0
- Molecular Formula: C28H24N4O2
- Molecular Weight: 448.516
- Catalog: Signaling Pathways Cell Cycle/DNA Damage Microtubule/Tubulin
- Create Date: 2018-01-11 16:52:23
- Modify Date: 2024-02-01 10:34:15
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PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively.
| Name | PE859 |
|---|---|
| Synonyms |
1H-Indole, 6-[(E)-2-[3-[(E)-2-[2-methoxy-4-(2-pyridinylmethoxy)phenyl]ethenyl]-1H-pyrazol-5-yl]ethenyl]-
6-[(E)-2-(3-{(E)-2-[2-Methoxy-4-(2-pyridinylmethoxy)phenyl]vinyl}-1H-pyrazol-5-yl)vinyl]-1H-indole |
| Description | PE859 is a potent inhibitor of both tau and Aβ aggregation with IC50 values of 0.66 and 1.2 μM, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.66 μM (tau), 1.2 μM (Aβ)[1] |
| In Vitro | 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 formation of beta-sheet structure[2]. |
| 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] |
| Kinase Assay | Tau aggregation is monitored using thioflavin T. The test compound (PE859), 10 μM 3RMBD and 10 μM heparin are dissolved in 50 mM Tris-HCl (pH7.6), and incubated at 37°C up to 144 hours. At each point of incubation time, 135 μL of the solutions are removed and mixed with 15 μL of 100 μM ThT solution (final concentration: 10 μM) and the fluorescence intensity with excitation at 440 nm and emission at 486 nm is measured[2]. |
| Animal Admin | Mice: PE859 is dissolved in 80% PEG400 and 20% water solution at 5 mg/mL, and orally-administered at a dose of 40 mg/kg/day for 6 months (from 9 to 15 months of age). The body weights of the mice are measured once a week during PE859 treatment[2]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 747.7±60.0 °C at 760 mmHg |
| Molecular Formula | C28H24N4O2 |
| Molecular Weight | 448.516 |
| Flash Point | 249.8±23.1 °C |
| Exact Mass | 448.189911 |
| LogP | 5.47 |
| Vapour Pressure | 0.0±2.4 mmHg at 25°C |
| Index of Refraction | 1.768 |
| Storage condition | 2-8℃ |