中文名称: | Amitifadine hydrochloride | ||||
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英文名称: | Amitifadine hydrochloride | ||||
别名: | DOV-21947 hydrochloride; EB-1010 hydrochloride;(1R,5S)-1-(3,4-Dichlorophenyl)-3-azabicyclo(3.1.0)hexane hydrochloride | ||||
CAS No: | 410074-74-7 | 分子式: | C11H12Cl3N | 分子量: | 264.58 |
CAS No: | 410074-74-7 | ||||
分子式: | C11H12Cl3N | ||||
分子量: | 264.58 |
基本信息
产品编号: |
A12754 |
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产品名称: |
Amitifadine hydrochloride |
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CAS: |
410074-74-7 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量 |
264.58 |
-20℃ |
1个月 |
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化学名: |
(1R,5S)-1-(3,4-Dichlorophenyl)-3-azabicyclo(3.1.0)hexane hydrochloride |
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Solubility (25°C): |
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体外:
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DMSO |
≥ 100 mg/mL (377.96mM) |
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Ethanol |
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Water |
50 mg/mL (188.98mM; Need ultrasonic) |
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体内(现配现用): |
1.请依序添加每种溶剂:10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.75 mg/mL (10.39mM); Clear solution |
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此方案可获得 ≥ 2.75 mg/mL (10.39mM,饱和度未知) 的澄清溶液。以 1mL 工作液为例,取 100μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50μL Tween-80,混合均匀;然后继续加入 450μL生理盐水定容至 1mL |
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2.请依序添加每种溶剂: 10% DMSO→ 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.75 mg/mL (10.39mM); Clear solution |
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此方案可获得 ≥ 2.75 mg/mL (10.39mM,饱和度未知) 的澄清溶液。以 1mL 工作液为例,取 100μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 |
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3.请依序添加每种溶剂: 10% DMSO→90% corn oil Solubility: ≥ 2.75 mg/mL (10.39mM); Clear solution |
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此方案可获得 ≥ 2.75 mg/mL (10.39mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。以 1mL 工作液为例,取 100μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900μL玉米油中,混合均匀。 |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
3.7796mL |
18.8979mL |
37.7958mL |
5mM |
0.7559mL |
3.7796mL |
7.5592mL |
10mM |
0.3780mL |
1.8898mL |
3.7796mL |
生物活性
产品描述 |
一种5-羟色胺-去甲肾上腺素-多巴胺的再摄取抑制剂 (SNDRI)。 |
靶点 |
IC50: 12nM (serotonin), 23nM (norepinephrine), 96nM (dopamine) |
体外研究 |
Amitifadine (DOV 21,947) is an antidepressant drug. Ki values for SERT, NET, and DAT are 99nM, 262nM, and 213nM. The IC 50 values for serotonin, norepinephrine and dopamine uptake are 12, 23 and 96nM, respectively |
体内研究 |
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 |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )