產品描述: | J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB). J-147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. J-147 has potential for the treatment of Alzheimer’s disease (AD) |
靶點: |
MAO B; Dopamine transporter;EpigeneticReaderDomain;?DopamineReceptor;?MonoamineOxidase |
體外研究: |
J-147 promotes HT22 and primary cell survival in a dose-dependent manner (EC50 value range of 0.06-0.115 μM) |
體內研究: |
J-147 (diet is prepared by the addition of J-147 at 200ppm; 6 months) enhances memory and dendritic spine number in old mice. The half life (t1/2) of J-147 is calculated at 1.5 hrs in plasma and 2.5 hrs in brain ( per oral (PO) administration at a single dose of 20 mg/kg). Animal Model: 24 male C57Bl/6 mice aged 24 months; using 8 month-old mice as controls Dosage: 200 ppm Administration: The diet was prepared by the addition of 200ppm; 6 months Result: While both young and old animals recognized when an object was moved a large distance (135 degrees), a reduction in the recognition index (RI) in aged mice was observed when the object was moved a smaller distance of 45 degrees. The reduction in the RI was reversed upon treatment with J147. |
參考文獻: |
1. Wang M, et al. The first synthesis of [11C]J147, a new potential PET agent for imaging of Alzheimer's disease. Bioorg Med Chem Lett. 2013 Jan 15;23(2):524-7. 2. Prior M, et al. The neurotrophic compound J147 reverses cognitive impairment in aged Alzheimer's disease mice. Alzheimers Res Ther. 2013 May 14;5(3):25. 3. Chen Q, et al. A novel neurotrophic drug for cognitive enhancement and Alzheimer's disease. PLoS One. 2011;6(12):e27865. 4. Prior M, et al. Selecting for neurogenic potential as an alternative for Alzheimer's disease drug discovery. Alzheimers Dement. 2016 Jun;12(6):678-86. |
溶解性: |
soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.854 ml |
14.272 ml |
28.544 ml |
5 mM |
0.571 ml |
2.854 ml |
5.709 ml |
10 mM |
0.285 ml |
1.427 ml |
2.854 ml |
50 mM |
0.057 ml |
0.285 ml |
0.571 ml |
|
注意: |
部分產品我司僅能提供部分信息,我司不保證所提供信息的權威性,僅供客戶參考交流研究之用。 |