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

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.

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TrkB activator-1

TrkB activator-1 Chemical Structure

CAS No. : 3087336-56-6

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Description

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

 

In Vitro

TrkB activator-1 (Compound B11) (3-100 100 μM, 24 h) increases the neurite total length, total count, and cross point count of hippocampal neurons[1].
TrkB activator-1 (1-100 100 μM, 0.25-2 h) upregulates BDNF in a dose-dependent manner in hippocampal neurons[1].
TrkB activator-1 (3-100 100 μM, 15 mins) increases the levels of p-TrkB, p-PLCγ, PKA and p-CREB in hippocampal neurons[1].

MedChemExpress (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.
In Vivo

TrkB activator-1 (Compound B11) (7.5-100 mg/kg, p.o., a single dose) induces a rapid-acting antidepressant effect in the chronic unpredictable mild stress (CUMS) mice models[1].

MedChemExpress (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.
Molecular Weight

268.33

Formula

C13H16D3N3O3

CAS No.
SMILES

O=C(N[C@H](C1=NC=CO1)C(C)C)[C@H]2CCN2C(C([2H])([2H])[2H])=O

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Purity & Documentation
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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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TrkB activator-1
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HY-175483S
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