计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
2-8°C储存,干燥。低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Amitifadine hydrochloride is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) , with IC 50 s of 12, 23, 96 nM for serotonin, norepinephrine and dopamine in HEK 293 cells , respectively.
In Vitro
Amitifadine (DOV 21,947) is an antidepressant drug. K i values for SERT, NET, and DAT are 99 nM, 262 nM, and 213 nM. The IC 50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The 30 mg/kg Amitifadine dose significantly reduces nicotine self-administration. The 5 and 10 mg/kg doses reduce nicotine self-administration during the first 15 min. of the session when the greatest amount of nicotine is self-administered. The 30 mg/kg Amitifadine dose, but not the lower doses cause a significant reduction in locomotor activity averaged over the 1-hour session and reduce food motivated responding. The 10 mg/kg dose causes hypoactivity at the beginning of the session, but 5 mg/kg does not cause any hypoactivity. The effect of chronic Amitifadine treatment (10 mg/kg) over the course of 15 sessions is also determined. Amitifadine causes a significant reduction in nicotine self-administration, which is not seen to diminish over two consecutive weeks of treatment and a week after enforced abstinence. Amitifadine significantly reduces nicotine self-administration. This prompts further research to determine if Amitifadine might be an effective treatment for smoking cessation. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Form:Solid
IC50& Target:IC50: 12 nM (serotonin), 23 nM (norepinephrine), 96 nM (dopamine)
规格
别名
盐酸阿米替拉定
规格或纯度
≥99%
英文名称
Amitifadine hydrochloride
生化机理
盐酸阿米替法汀是一种血清素-去甲肾上腺素-多巴胺再摄取抑制剂（SNDRI），在 HEK 293 细胞中对血清素、去甲肾上腺素和多巴胺的 IC 50 s 分别为 12、23 和 96 nM。
储存条件
2-8°C储存,干燥
运输条件
低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
技术文档
高级数据
关联靶点（人）
SLC6A2
Tclin
钠依赖性去甲肾上腺素转运体(Sodium-dependent noradrenaline transporter)
(2 活性数据)
SLC6A3
Tclin
钠依赖性多巴胺转运体(Sodium-dependent dopamine transporter)
(2 活性数据)
SLC6A4
Tclin
钠依赖性血清素转运体(Sodium-dependent serotonin transporter)
(2 活性数据)
SLC6A2
Tclin
Norepinephrine transporter
(10102 活性数据)
SLC6A4
Tclin
Serotonin transporter
(12625 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : ≥ 100 mg/mL (377.96 mM) H2O : 50 mg/mL (188.98 mM; Need ultrasonic)
分子量
264.600 g/mol
XLogP3
氢键供体数Hydrogen Bond Donor Count
2
氢键受体数Hydrogen Bond Acceptor Count
1
可旋转键计数Rotatable Bond Count
1
精确质量Exact Mass
263.004 Da
单同位素质量Monoisotopic Mass
263.004 Da
拓扑极表面积Topological Polar Surface Area
12.000 Ų
重原子数Heavy Atom Count
15
形式电荷Formal Charge
0
复杂度Complexity
245.000
同位素原子数Isotope Atom Count
0
定义的原子立体中心计数Defined Atom Stereocenter Count
2
未定义的原子立体中心计数Undefined Atom Stereocenter Count
0
定义的键立体中心计数Defined Bond Stereocenter Count
0
未定义的键立体中心计数Undefined Bond Stereocenter Count
0
所有立体化学键的总数The total count of all stereochemical bonds
0
共价键合单元计数Covalently-Bonded Unit Count
2
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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