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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 3087336-56-6
- 分子式: C13H16D3N3O3
- 分子量:268.33
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
IC50 & Target
[1]|
TrkB |
体外実験
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 % |
体内実験
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.
アプリケーション
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.
化学情報
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CAS 番号 3087336-56-6
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非標識Cas 3087336-92-0
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分子量 268.33
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TrkB activator-1 関連分類
HY-175483S 関連分類
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