- ￥2128 - 13840
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- T32737
- 2026年07月07日
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- CAS号：
1198790-53-2
- 规格：
1mg/5mg/10mg/25mg/50mg
| 规格： | 1mg | 产品价格： | ￥2128.0 |
|---|---|---|---|
| 规格： | 5mg | 产品价格： | ￥5080.0 |
| 规格： | 10mg | 产品价格： | ￥6944.0 |
| 规格： | 25mg | 产品价格： | ￥10320.0 |
| 规格： | 50mg | 产品价格： | ￥13840.0 |
Product Introduction
Bioactivity
| 名称 | Liafensine |
| 描述 | Liafensine(BMS-820836) is a novel and selective triple monoamine reuptake inhibitor with inhibitory effects on the reuptake of serotonin, norepinephrine, and dopamine for the study of major depressive disorder and central nervous system disorders. |
| 体内活性 | Healthy subjects were assigned to seven BMS-820836 dose panels (0.025, 0.1, 0.5, 1, 2, 3, and 5 mg; n = 8 each), in which subjects were randomly allocated 3:1 to a single BMS-820836 dose or matched placebo. Serial blood samples were collected on Days 1, 2, 3, 4, 7, and 14 to characterize the PK of BMS-820836. Following evaluation of the maximum tolerated dose, SERT occupancy was determined by applying [(11)C]DASB positron emission tomography (PET) after single-dose BMS-820836 (0.5 or 3 mg; n = 3 each) and DAT occupancy by applying [(11)C]PE2I PET after single-dose BMS-820836 (3 mg; n = 6). RESULTS: Single oral doses of BMS-820836 (0.025-3 mg) were generally safe and well tolerated. BMS-820836 had a median T max of 5.0-7.2 h and a mean apparent terminal T 1/2 of 34-57 h. Mean striatal SERT occupancies were 19 ± 9 % and 82 ± 8 % after single doses of 0.5 and 3 mg BMS-820836, respectively. The mean striatal DAT occupancy was 19 ± 9 % after a single 3 mg BMS-820836 dose. CONCLUSIONS: Single doses of BMS-820836 have meaningful SERT and DAT occupancy and demonstrate an acceptable safety and tolerability profile in healthy control subjects.[1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | DMSO : 33.33 mg/mL (90.95 mM), Sonication is recommended. |
| 关键字 | serotonin reuptake | norepinephrine reuptake | Liafensine | DopamineReceptor | dopamine reuptake | Dopamine Receptor | DB-104 | DB 104 | 5HTReceptor | 5HT Receptor |
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| 相关库 | Inhibitor Library | Angiogenesis related Compound Library | Bioactive Compound Library | Bioactive Compounds Library Max | ReFRAME Related Library | Neurotransmitter Receptor Compound Library | Neuronal Signaling Compound Library | GPCR Compound Library | Membrane Protein-targeted Compound Library | Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Pain-Related Compound Library |
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￥2128 - 13840
