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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- CAS. Nr.: 3087336-56-6
- Formel: C13H16D3N3O3
- Molecular Weight:268.33
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
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Help & FAQs
Biologische Aktivität
Beschreibung
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.
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Cell Line:Hippocampal neurons
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Concentration:3, 10,30 and 100 μM
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Incubation Time:15 mins
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Result:Increased PKA and p-CREB levels.
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | Cmax | AUClast | F |
|---|---|---|---|---|---|---|---|---|
| Dog[1] | 3 mg/kg | i.v. | 3.4 mL/min/kg | 0.65 L/kg | / | / | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | 2.03 h | 5255 ng/mL | 26803 ng·h/mL | 110 % |
| Mice[1] | 10 mg/kg | i.v. | 24.2 mL/min/kg | 1.81 L/kg | / | / | / | / |
| Mice[1] | 15 mg/kg | p.o. | / | / | 1.63 h | 5667 ng/mL | 17122 ng·h/mL | 160 % |
| Rat[1] | 10 mg/kg | i.v. | 6.5 mL/min/kg | 0.57 L/kg | / | / | / | / |
| Rat[1] | 15 mg/kg | p.o. | / | / | 1.82 h | 5753 ng/mL | 24315 ng·h/mL | 66 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chronic unpredictable mild stress (CUMS) mice models[1]
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Dosage:7.5, 15, 25, 50 and 100 mg/kg
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Administration:Oral administration
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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.
Anwendung
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS. Nr. 3087336-56-6
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Unlabeled CAS 3087336-92-0
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Molecular Weight 268.33
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Formel C13H16D3N3O3
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SMILES
O=C(N[C@H](C1=NC=CO1)C(C)C)[C@H]2CCN2C(C([2H])([2H])[2H])=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
TrkB activator-1 Related Classifications
HY-175483S Related Classifications
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