Clozapine N-oxide dihydrochloride 氯氮平N-氧化盐酸,98.17%

产品编号:Bellancom-17366A| CAS NO:2250025-93-3| 分子式:C18H21Cl3N4O| 分子量:415.74

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-17366A
750.00 杭州 北京(现货)
Bellancom-17366A
1100.00 杭州 北京(现货)

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Clozapine N-oxide dihydrochloride 氯氮平N-氧化盐酸

产品介绍 Clozapine N-oxide dihydrochloride 是一种 Clozapine 的主要代谢产物,也是一种人毒蕈碱设计受体 (DREADDs) 激动剂。Clozapine N-oxide dihydrochloride 可激活 DREADD 受体 hM3DqhM4Di。Clozapine N-oxide dihydrochloride 可以穿过血脑屏障。Clozapine 是一种有效的多巴胺拮抗剂,也一种是有效的选择性毒蕈碱 M4 受体 (muscarinic M4 receptor) (EC50 为 11 nM) 激动剂。
生物活性

Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier[4]. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist[5][6].

体外研究

Clozapine N-oxide (CNO) can bind to non-DREADD receptors at concentrations required for DREADD activation, and undergoes reverse-metabolism to its parent compound clozapine, an atypical antipsychotic that acts at a variety of pharmacological targets and produces numerous physiological and behavioral effects.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

After a single intraperitoneal (i.p.) injection of Clozapine N-oxide (1 mg/kg) into mice, Clozapine N-oxide (CNO) plasma levels peak at 15 min and are very low after 2 h. Despite the short plasma half-life of CNO in mice, the biological effects that have been described after acute treatment of DREADD-expressing experimental animals are usually much longer (6-10 h).

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状Solid
溶解性数据
In Vitro: 

DMSO : 240 mg/mL (577.28 mM; Need ultrasonic)

H2O : 100 mg/mL (240.53 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4053 mL 12.0267 mL 24.0535 mL
5 mM 0.4811 mL 2.4053 mL 4.8107 mL
10 mM 0.2405 mL 1.2027 mL 2.4053 mL
*

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
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 6 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 6 mg/mL (14.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 60.0 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50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 6 mg/mL (14.43 mM); Clear solution

    此方案可获得 ≥ 6 mg/mL (14.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 60.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

参考文献

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