| Bioactivity | J-147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J-147 can readily pass the blood brain barrier (BBB)[1]. 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[2]. J-147 has potential for the treatment of Alzheimer’s disease (AD)[3]. | ||||||||||||
| Target | MAO B; Dopamine transporter | ||||||||||||
| Invitro | J-147 promotes HT22 and primary cell survival in a dose-dependent manner (EC50 value range of 0.06-0.115 μM) [2]. | ||||||||||||
| In Vivo | J-147 (diet is prepared by the addition of J-147 at 200ppm; 6 months) enhances memory and dendritic spine number in old mice[4].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)[2]. Animal Model: | ||||||||||||
| Name | J-147 | ||||||||||||
| CAS | 1146963-51-0 | ||||||||||||
| Formula | C18H17F3N2O2 | ||||||||||||
| Molar Mass | 350.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |