Bioactivity | TrkB-IN-1 is a potent and orally active TrkB agonist and has favorable PK properties. TrkB-IN-1 reverses the cognitive defects in an AD mouse model and can be used for alzheimer’s disease research[1]. |
In Vivo | TrkB-IN-1 (oral gavage; 7.25 mg/kg, 21.8 mg/kg, 43.6 mg/kg; 3 month) 在 5XFAD 小鼠中以剂量依赖性方式激活小鼠海马中的 TrkB 信号级联,p-TrkB/TrkB、p-Akt/Akt 和 p-ERK/ERK 的比值也增加[1]。TrkB-IN-1 (oral gavage; 7.25 mg/kg, 21.8 mg/kg, 43.6 mg/kg; 5 days) 可减轻 5XFAD 小鼠的 Aβ 沉积并恢复记忆缺陷[1]。TrkB-IN-1 (oral gavage; 36 mg/kg) 的口服生物利用度为 10.5%,Cmax 为 129 ng/mL, Tmax 为 0.5 h, T1/2 为 3.66 h[1]。 |
Name | TrkB-IN-1 |
CAS | 1609067-49-3 |
Formula | C19H16N2O6 |
Molar Mass | 368.34 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Chun Chen, et al. The prodrug of 7,8-dihydroxyflavone development and therapeutic efficacy for treating Alzheimer's disease. Proc Natl Acad Sci U S A. 2018 Jan 16;115(3):578-583. |