S82107 |
J-147 |
源叶(MedMol) | 98% |
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- 产品描述: 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)
- 靶点: MAO B; Dopamine transporter;EpigeneticReaderDomain; DopamineReceptor; MonoamineOxidase
- 体外研究:
J-147 promotes HT22 and primary cell survival in a dose-dependent manner (EC50 value range of 0.06-0.115 μM)
- 体内研究:
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.
- 参考文献:
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
- 保存条件: -20℃
- 配置溶液浓度参考:
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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)