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N-Desmethylclozapine

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产品编号 T5158Cas号 6104-71-8
别名 N-去甲基氯氮平, Normethylclozapine, Norclozapine, Desmethylclozapine

N-Desmethylclozapine (Desmethylclozapine) 是非典型抗精神病药 Clozapine 的主要活性代谢产物。它是血清素受体亚型 5-HT2C 的拮抗剂,IC50值为7.1 nM。 它也是多巴胺 D4 受体的拮抗剂和δ-阿片受体的激动剂。

N-Desmethylclozapine
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N-Desmethylclozapine

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纯度: 97.25%
产品编号 T5158 别名 N-去甲基氯氮平, Normethylclozapine, Norclozapine, DesmethylclozapineCas号 6104-71-8

N-Desmethylclozapine (Desmethylclozapine) 是非典型抗精神病药 Clozapine 的主要活性代谢产物。它是血清素受体亚型 5-HT2C 的拮抗剂,IC50值为7.1 nM。 它也是多巴胺 D4 受体的拮抗剂和δ-阿片受体的激动剂。

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1 mg
¥ 155
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5 mg
¥ 353
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10 mg
¥ 597
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25 mg
¥ 1,360
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50 mg
¥ 2,150
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100 mg
¥ 3,110
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200 mg
¥ 4,380
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1 mL x 10 mM (in DMSO)
¥ 437
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产品介绍

生物活性
产品描述
N-Desmethylclozapine (Desmethylclozapine) is an antagonist of serotonin (5-HT) receptor subtype 5-HT2C (IC50: 7.1 nM). It also is an antagonist at dopamine D4 receptors, an agonist at δ-opioid receptors.
靶点活性
5-HT2C:7.1 nM
体外活性
N-desmethylclozapine antagonized 5-HT-stimulated phosphoinositide hydrolysis with IC50 values of 29.4 nM [1]. N-desmethylclozapine exhibited slight agonistic effects on the M1 mAChR and agonistic properties at the 5-HT1A receptor in the cerebral cortex and hippocampus. This compound also behaved as an agonist at the δ-opioid receptor in the cerebral cortex and the striatum [2]. Muscarinic agonist activity of N-desmethylclozapine was higher than that of clozapine, higher in excitatory neurons than in inhibitory neurons, sensitive to pirenzepine, and partially masked when co-applied with clozapine [3].
体内活性
NDMC (3-30mg/kg) decreased exploratory locomotor activity in a dose-dependent manner, and the reduced locomotor activity was significantly antagonized by scopolamine at doses of 0.1 and 0.3mg/kg. NDMC (10-30mg/kg) dose-dependently increased prepulse inhibition (PPI) in DBA/2J mice [4].
动物实验
Exploratory locomotor activity was monitored as described previously. Animals were habituated to the experimental room for at least 60 min before testing. Oxotremorine (0.01, 0.03, 0.1 mg/kg, s.c.), NDMC (3, 10, 30 mg/kg, s.c.), xanomeline (0.3, 1, 3 mg/kg, s.c.), or scopolamine (0.1, 0.3, 1 mg/kg, s.c.) was administered. Scopolamine (0.1, 0.3 mg/kg, s.c.) was injected 30 min before the administration of test agents in antagonism studies. Animals were placed in plastic cages (22.5D×33.8 W×14.0H cm) immediately after the administration of test agents in the antagonism studies, and exploratory locomotor activity was measured during a 60 min observation period using an infrared motion detector system [4].
别名N-去甲基氯氮平, Normethylclozapine, Norclozapine, Desmethylclozapine
化学信息
分子量312.8
分子式C17H17ClN4
CAS No.6104-71-8
SmilesClc1ccc2N=c3ccccc3=C(Nc2c1)N1CCNCC1
密度1.38g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 50 mg/mL (159.85 mM), Sonication is recommended.
Ethanol: 30 mg/mL (95.91 mM), Sonication is recommended.
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM3.1969 mL15.9847 mL31.9693 mL159.8465 mL
5 mM0.6394 mL3.1969 mL6.3939 mL31.9693 mL
10 mM0.3197 mL1.5985 mL3.1969 mL15.9847 mL
20 mM0.1598 mL0.7992 mL1.5985 mL7.9923 mL
50 mM0.0639 mL0.3197 mL0.6394 mL3.1969 mL
DMSO
1mg5mg10mg50mg
100 mM0.0320 mL0.1598 mL0.3197 mL1.5985 mL

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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 20 g ,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% ddH2O. 那么您的工作液浓度为 2 mg/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 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | 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。

1 请输入动物实验的基本信息
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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
%
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%ddH2O

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