Gambogic amide 是一种有效的选择性 TrkA 激动剂，还诱导其酪氨酸磷酸化和下游信号传导激活，包括 Akt 和 MAPK。Gambogic amide 能够特异性地与 TrkA 受体的细胞质近膜结构域相互作用并触发其二聚化，使致激活。 Gambogic amide 具有神经保护活性可防止谷氨酸诱导的神经元细胞死亡。Gambogic amide 在中风短暂性大脑中动脉闭塞模型中具有改善效力，可用于研究神经退行性疾病和中风。
| 生物活性 |
Gambogic amide is a potent and selective agonist of TrkA and also induces its tyrosine phosphorylation and activation of downstream signaling, including Akt and MAPK. Gambogic amide specifically interacts with the cytoplasmic juxtamembrane domain of the TrkA receptor and triggers its dimerization, leading to activation. Gambogic amide has neuroprotective activity preventing glutamate-induced neuronal cell death. Gambogic amide has improved efficacy in a transient middle cerebral artery occlusion model of stroke and could be used to study neurodegenerative diseases and stroke |
|---|---|
| 分子式 |
C38H45NO7
|
| 分子量 |
627.77
|
| CAS号 |
286935-60-2
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Store at -20˚C |
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