1. Neuronal Signaling Protein Tyrosine Kinase/RTK Others
  2. Trk Receptor Isotope-Labeled Compounds
  3. TrkB activator-1

TrkB activator-1 是一种特异性、具有口服活性且能穿透血脑屏障的原肌球蛋白受体激酶 B (TrkB) 激活剂。TrkB activator-1 通过激活脑源性神经营养因子 (BDNF)-原肌球蛋白相关激酶 B (TrkB)-环磷酸腺苷反应元件结合蛋白 (CREB) 信号轴,显示出强效的抗抑郁作用。TrkB activator-1 能增强神经可塑性。TrkB activator-1 可用于神经系统疾病的研究,如抑郁症。

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TrkB activator-1

TrkB activator-1 Chemical Structure

CAS No. : 3087336-56-6

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生物活性

TrkB activator-1 is a specific, orally active and brain-penetrant tropomyosin receptor kinase B (TrkB) activator. TrkB activator-1 shows potent antidepressant effects through activation of the activates the BDNF (brainderived neurotrophic factor)-Tropomyosin-related kinase B (TrkB)-CREB (cAMP response element binding protein) signaling aixs. TrkB activator-1 increaes neuroplasticity. TrkB activator-1 can be used for the research of neurological disease, such as depression[1].

IC50 & Target[1]

TrkB

 

体外研究
(In Vitro)

TrkB activator-1 (Compound B11) (3-100 100 μM, 24 h) 可增加海马神经元的神经突总长度、总数量和交叉点数量[1]
TrkB activator-1 (1-100 100 μM, 0.25-2 h) 以剂量依赖的方式上调海马神经元中的 BDNF[1]
TrkB activator-1 (3-100 100 μM, 15 mins) 可增加海马神经元中 p-TrkB、p-PLCγ、PKA 和 p-CREB 的水平[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: 3, 10,30 and 100 μM
Incubation Time: 15 mins
Result: Increased PKA and p-CREB levels.
体内研究
(In Vivo)

TrkB activator-1 (Compound B11) (7.5-100 mg/kg,口服,单剂量) 在慢性不可预知温和应激致抑郁小鼠模型中诱导出快速起效的抗抑郁作用[1]

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

Animal Model: Chronic unpredictable mild stress (CUMS) mice models[1]
Dosage: 7.5, 15, 25, 50 and 100 mg/kg
Administration: Oral administration
Result: Showed a fast-onset remission of the depressive behavior.
Upregulated the number of action potential events in the tissue of the hippocampus and dorsal raphe nucleus.
Led to significantly reduced immobility time in the TST and FST.
Exhibited marked upregulation of BDNF, cAMP, and CREB level.
Increased dendritic spines in hippocampus and PFC.
分子量

268.33

Formula

C13H16D3N3O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • 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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TrkB activator-1
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HY-175483S
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