1. Neuronal Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  2. Trk Receptor Akt ERK
  3. Gambogic amide

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。

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Gambogic amide Chemical Structure

Gambogic amide Chemical Structure

CAS No. : 286935-60-2

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  • 参考文献

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[1].

体外研究
(In Vitro)

Gambogic amide(0.5 μM;30 分钟)可引发海马神经元中的 TrkA 酪氨酸磷酸化[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Hippocampal neurons
Concentration: 500 nM
Incubation Time: 30 min
Result: Triggered TrkA Y490 phosphorylation.
体内研究
(In Vivo)

Gambogic amide(2 mg/kg;皮下注射;单剂量)可防止 MCAO 动物模型中的神经细胞死亡并减少梗塞体积[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: MCAO mice model[1]
Dosage: 2 mg/kg
Administration: s.c.; 5 min before the onset of reperfusion, after 2 h of MCAO followed by reperfusion; followed by 25 mg/kg Kainic acid (KA)
Result: Diminished Kainic acid-triggered hippocampal neuronal cell death.
Reduces infarct volume in MCAO rat brain.
分子量

627.77

Formula

C38H45NO7

CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Gambogic amide
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HY-121833
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