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Vortioxetine hydrobromide (Lu AA21004 hydrobromide) 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和5-羟色胺转运体(SERT)的抑制剂,Ki 值分别为 15、33、3.7、19 和 1.6 nM。
Vortioxetine hydrobromide (Lu AA21004 hydrobromide) 是5-HT1A、5-HT1B、5-HT3A、5-HT7受体和5-羟色胺转运体(SERT)的抑制剂,Ki 值分别为 15、33、3.7、19 和 1.6 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥ 153 | 现货 | |
10 mg | ¥ 248 | 现货 | |
25 mg | ¥ 395 | 现货 | |
50 mg | ¥ 548 | 现货 | |
100 mg | ¥ 738 | 现货 | |
200 mg | ¥ 1,180 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 273 | 现货 |
产品描述 | Vortioxetine hydrobromide (Lu AA21004 hydrobromide) is a serotonin (5-HT) modulator and stimulator (SMS), inhibits 5-HT1A/1B/3A/7 receptor and SERT (IC50: 15/33/3.7/19/1.6 nM). |
靶点活性 | SERT:1.6nM, 5-HT7:19nM, 5-HT11B:33nM, 5-HT13A:3.7nM, 5-HT1A:15nM |
体外活性 | 皮下注射Lu AA21004(2.5-10.0 mg/kg)到大鼠的内侧前额叶皮层和腹侧海马区,可使细胞外5-HT,DA和NA的水平提高.皮下注射Lu AA21004(5 mg/kg)到大鼠的腹侧海马区,可提高细胞外5-HT水平 (200%).注射Lu AA21004(5 和10 mg/kg)20分钟后,ACh的水平得到提高,分别提高至224%和204%.Lu-AA21004(5 和10 mg/kg)到清醒大鼠腹侧的海马区,增强细胞外5-HT的水平.Lu-AA21004(5 和10 mg/kg)处理内侧前额叶皮层3天后,使5-HT的基础水平明显提高.Lu AA21004(10 mg/kg)可使大鼠的痛觉明显降低.在大鼠体内,Lu-AA21004的肝脏清除力及口服生物有效性分别为7.1(L/h)/kg和16%.Lu AA21004剂量依赖性影响大鼠的Bezold-Jarisch反射,抑制短暂的心动过缓(ED50:0.11 mg/kg). |
体内活性 | Lu AA21004是h5-HT1B受体激动剂(EC50:460 nM),全细胞检测中内在活性为22%。Lu-AA21004抑制重组人类CYP1A2(IC50:40 μM),CYP2C9(IC50:39 μM), CYP2D6(IC50:9.8 μM)和CYP3A4(IC50:10 μM)。在体外全细胞cAMP检测中,Lu AA21004结合到r5-HT7受体上(Ki:200 nM)。Lu AA21004是r5-HT7受体的一种功能性拮抗剂(IC50:2 μM)。 |
激酶实验 | Assay of MEK Kinase Activity: Anti-MEK1 antibody is used to immunoprecipitate MEK1 molecules. MEK kinase activity is measured as the ability of immuno-isolated MEK1 to activate recombinant ERK1 in a coupled assay using MBP as the end point of the assay. Phosphorylated MBP is resolved on a 14% SDS-PAGE gel and vacuum-dried before exposure to X-ray film. |
别名 | 盐酸沃替西汀, 氢溴酸沃替西汀, Vortioxetine (Lu AA21004) HBr, Vortioxetine HBr, Lu AA21004 hydrobromide |
分子量 | 379.36 |
分子式 | C18H22N2S·HBr |
CAS No. | 960203-27-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | Ethanol: 14 mg/mL (36.9 mM) DMSO: 45 mg/mL (118.62 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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