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Dextromilnacipran

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纯度: 99.5%

货号 T2594Cas号 96847-55-1

别名 左旋米那普仑, Levomilnacipran

Dextromilnacipran (Levomilnacipran) 是米那普仑的对映体,是一种选择性 5- 羟色胺和去甲肾上腺素(5-HT/NE)再摄取抑制剂,也是一种人类 α 肾上腺素能受体拮抗剂,IC50=3.4 μM。

Dextromilnacipran
其他形式的 “Dextromilnacipran”:
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Dextromilnacipran

一键复制产品信息
Rating icon 很棒

纯度: 99.5%

货号 T2594 别名 左旋米那普仑, LevomilnacipranCas号 96847-55-1

Dextromilnacipran (Levomilnacipran) 是米那普仑的对映体,是一种选择性 5- 羟色胺和去甲肾上腺素(5-HT/NE)再摄取抑制剂,也是一种人类 α 肾上腺素能受体拮抗剂,IC50=3.4 μM。

规格价格库存数量
1 mg
¥ 198
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5 mg
¥ 448
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10 mg
¥ 776
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25 mg
¥ 1,550
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50 mg
¥ 2,290
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100 mg
¥ 3,430
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500 mg
¥ 7,470
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1 mL x 10 mM (in DMSO)
¥ 565
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产品介绍


Dextromilnacipran AI Summary
**Dextromilnacipran** is a pharmacologically active compound primarily studied for its interactions with neurotransmitter transporters, demonstrating significant inhibition of the norepinephrine transporter (NET) and moderate inhibition of the serotonin transporter (SERT). It exhibits potent inhibition of human NET with an IC50 as low as 77.0 nM and moderate inhibition of human SERT with IC50 values ranging between 100.0 nM and 420.0 nM across different studies. The compound shows weaker inhibition of the dopamine transporter (DAT) with an IC50 of 6100.0 nM. Pharmacokinetically, Dextromilnacipran has high oral bioavailability in humans at 84%, with a rapid Tmax of 2.0 hours and a moderate half-life of 8.0 hours. It demonstrates moderate protein binding in human plasma (13.0%) and significant excretion activity in human urine (>80.0%). The compound shows metabolic stability in both human and rat liver microsomes, with clearance values of 3.1 mL.min-1.kg-1 and 24.0 mL.min-1.kg-1 respectively, and exhibits low affinity for P-glycoprotein-mediated transport. Additionally, it has a Log D value of 0.2, indicating moderate lipophilicity, and shows favorable permeability in Caco-2 cell lines. Despite its effective bioactivity, Dextromilnacipran exhibits moderate liver toxicity, indicated by a severity class index of 7.0 for drug-induced liver injury, and shows potential hepatotoxic effects without significant chronic liver disease or tumor formation. Overall, Dextromilnacipran holds promise for modulating neurotransmitter transporters, especially NET and SERT, with potential therapeutic implications and significant pharmacokinetic and pharmacodynamic profiles that warrant further investigation..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Dextromilnacipran (Levomilnacipran) is a selective serotonin and norepinephrine reuptake inhibitor.
靶点活性
α-adrenoceptor:3.4 μM (IC50)
别名左旋米那普仑, Levomilnacipran
化学信息
分子量246.35
分子式C15H22N2O
CAS No.96847-55-1
SmilesC(N(CC)CC)(=O)[C@]1([C@@H](CN)C1)C2=CC=CC=C2
密度1.077
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 250 mg/mL (1014.82 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM4.0593 mL20.2963 mL40.5927 mL202.9633 mL
5 mM0.8119 mL4.0593 mL8.1185 mL40.5927 mL
10 mM0.4059 mL2.0296 mL4.0593 mL20.2963 mL
20 mM0.2030 mL1.0148 mL2.0296 mL10.1482 mL
50 mM0.0812 mL0.4059 mL0.8119 mL4.0593 mL
100 mM0.0406 mL0.2030 mL0.4059 mL2.0296 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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