Liafensine
Liafensine (BMS-820836) is an orally active, blood-brain barrier-permeable monoamine reuptake inhibitor, with an IC50 of 5.67 nM against DAT, 1.08 nM against SERT, and 7.99 nM against NET. Liafensine binds to DAT to block dopamine reuptake. Liafensine binds to SERT to block serotonin reuptake. Liafensine binds to NET to block norepinephrine reuptake. Liafensine can be used in studies related to depression.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 1198790-53-2
- 分子式: C24H22N4
- 分子量:366.46
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
IC50: 1.08 nM (serotonin transporter), 5.67 nM (dopamine transporter), 7.99 nM (norepinephrine transporter)
体外実験
Liafensine potently inhibits monoamine reuptake in embryonic kidney 293 cells expressing SERT, DAT and NET, with IC50 values of 1.08 nM, 5.67 nM and 7.99 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1198790-53-2
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性状 Solid
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分子量 366.46
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分子式 C24H22N4
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Color Light yellow to brown
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SMILES
NC1=NN=C(C2=CC3=C(C=C2)[C@H](C4=CC=C5C=CC=CC5=C4)CN(C)C3)C=C1
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別名
BMS-820836
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
純度とドキュメンテーション
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データシート (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Risinger R, et al. Evaluation of safety and tolerability, pharmacokinetics, and pharmacodynamics of BMS-820836 in healthy subjects: a placebo-controlled, ascending single-dose study. Psychopharmacology (Berl). 2014 Jun;231(11):2299-310. [Content Brief]
[2]. Bhagwagar Z, et al. Assessment of the Efficacy and Safety of BMS-820836 in Patients With Treatment-Resistant Major Depression: Results From 2 Randomized, Double-Blind Studies. J Clin Psychopharmacol. 2015 Aug;35(4):454-9. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Liafensine 関連分類
HY-19907 関連分類
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Keywords
- Liafensine
- 1198790-53-2
- BMS-820836
- BMS820836
- BMS 820836
- Dopamine Transporter
- Monoamine Transporter
- Serotonin Transporter
- monoamine reuptake inhibitor
- human NET
- treatment-resistant major depression
- dopamine reuptake
- human embryonic kidney 293 cells
- human SERT
- serotonin reuptake
- norepinephrine reuptake
- blood-brain barrier
- human DAT
- Inhibitor
- inhibitor
- inhibit