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.
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- CAS No.: 1198790-53-2
- 화학식: C24H22N4
- 분자량:366.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
IC50: 1.08 nM (serotonin transporter), 5.67 nM (dopamine transporter), 7.99 nM (norepinephrine transporter)
In Vitro
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1198790-53-2
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Appearance Solid
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분자량 366.46
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화학식 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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Synonyms
BMS-820836
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Liafensine Related Classifications
HY-19907 Related Classifications
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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