2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Anti-infection
  3. mAChR Opioid Receptor Drug Metabolite Virus Protease
  4. N-Desmethylclozapine

N-Desmethylclozapine  (Synonyms: N-去甲基氯氮平; Norclozapine; Desmethylclozapine; Normethylclozapine)

目录号: HY-G0021 纯度: 98.99%
COA 产品使用指南

摩尔计算器

N-Desmethylclozapine 是非典型抗精神病有效剂 Clozapine 的主要活性代谢产物。N-Desmethylclozapine 是一种有效的、变构的部分 M1 受体激动剂 (EC50=115 nM)，能通过 M1 受体激活增强海马 N-methyl-d-aspartate (NMDA) 受体电流。N-Desmethylclozapine 也是 δ-opioid 激动剂。

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N-Desmethylclozapine Chemical Structure

N-Desmethylclozapine Chemical Structure

CAS No. : 6104-71-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥880
In-stock
5 mg ￥800
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10 mg ￥1400
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25 mg ￥3000
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Customer Review

Other Forms of N-Desmethylclozapine:

N-Desmethylclozapine 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist[1][2].

IC50 & Target

mAChR1

 

δ Opioid Receptor/DOR

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
BHK-21 EC50
170 nM
Compound: 3, NDMC
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M5 receptor expressed in BHK-21 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
[PMID: 20684563]
BHK-21 EC50
400 nM
Compound: 3, NDMC
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M4 receptor expressed in BHK-21 cells coexpressing Galpha16 subunit assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
[PMID: 20684563]
CHO-K1 EC50
140 nM
Compound: 3, NDMC
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M1 receptor Y381A mutant expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
[PMID: 20684563]
CHO-K1 EC50
18 nM
Compound: 3, NDMC
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
Agonist activity at human muscarinic M1 receptor expressed in CHO-K1 cells assessed as increase of acetylcholine-induced calcium flux by FLIPR assay
[PMID: 20684563]
体外研究
(In Vitro)

The brain penetrant metabolite N-desmethylclozapine preferentially bound to M1 muscarinic receptors with an IC50 of 55 nM and was a more potent partial agonist (EC50, 115 nM and 50% of acetylcholine response) at this receptor than clozapine[1].
N-desmethylclozapine exhibits slight agonistic effects on the M1 mAChR, and agonistic properties at the 5-HT1A receptor in the cerebral cortex and hippocampus. This compound also behaves as an agonist at the δ-opioid receptor in the cerebral cortex and striatum[2].
N-desmethylclozapine (3 μM) greatly decreases the outward current in excitatory neurons, but not in inhibitory neurons. In excitatory neurons, N-desmethylclozapine alone is more effective than either clozapine alone or the combination of clozapine and N-desmethylclozapine. The effect of N-desmethylclozapine in excitatory neurons is significantly suppressed by 0.1 μM pirenzepine and 1 μM atropine. N-desmethylclozapine, but not clozapine, suppressed K+ channels via M1 receptors in excitatory cells[3].
N-desmethylclozapine leads to a decrease in TxB2 levels under unstimulated conditions as well as under TSST-1 stimulation. Clozapine, N-desmethylclozapine and CPZ possibly act on neurotransmitter systems via modulation of TxA2 or TxB2 production[5].
The IC50s of N-desmethylclozapine, fluoxetine hydrochloride, and salmeterol xinafoate in Huh-7 cells infected with DENV-2 are 1 μM, 0.38 μM, and 0.67 μM, respectively. The levels of NS3 are reduced in cells treated with all three inhibitors compared to DMSO treatment, suggesting that the inhibitors act at a stage prior to viral protein translation. N-Desmethylclozapine-treated cells show a >75% reduction in negative-strand RNA levels[6].

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

N-Desmethylclozapine 相关抗体:
体内研究
(In Vivo)

N-desmethylclozapine in rat and human at M2 and M4 mAChRs underlying presynaptic modulation of GABA and glutamate release, respectively. In particular, N-desmethylclozapine maybe a M2 mAChR antagonist in the rat but has no activity at this receptor in human neocortex. However, N-desmethylclozapine has an agonistic effect at M4 mAChR in the human but no such effect in the rat neocortex[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

312.80

Formula

C17H17ClN4
CAS 号
性状

固体

颜色

Light yellow to green yellow

中文名称

氯氮平EP杂质C
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : ≥ 50 mg/mL (159.85 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1969 mL 15.9847 mL 31.9693 mL
5 mM 0.6394 mL 3.1969 mL 6.3939 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (7.99 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

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

    Solubility: ≥ 2.5 mg/mL (7.99 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 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。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 98.99%

COA (294 KB) LCMS (112 KB)

产品使用指南 (1538 KB)
参考文献

N-Desmethylclozapine 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1969 mL 15.9847 mL 31.9693 mL 79.9233 mL
5 mM 0.6394 mL 3.1969 mL 6.3939 mL 15.9847 mL
10 mM 0.3197 mL 1.5985 mL 3.1969 mL 7.9923 mL
15 mM 0.2131 mL 1.0656 mL 2.1313 mL 5.3282 mL
20 mM 0.1598 mL 0.7992 mL 1.5985 mL 3.9962 mL
25 mM 0.1279 mL 0.6394 mL 1.2788 mL 3.1969 mL
30 mM 0.1066 mL 0.5328 mL 1.0656 mL 2.6641 mL
40 mM 0.0799 mL 0.3996 mL 0.7992 mL 1.9981 mL
50 mM 0.0639 mL 0.3197 mL 0.6394 mL 1.5985 mL
60 mM 0.0533 mL 0.2664 mL 0.5328 mL 1.3321 mL
80 mM 0.0400 mL 0.1998 mL 0.3996 mL 0.9990 mL
100 mM 0.0320 mL 0.1598 mL 0.3197 mL 0.7992 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

N-Desmethylclozapine6104-71-8Norclozapine Desmethylclozapine Normethylclozapine氯氮平EP杂质CmAChROpioid ReceptorDrug MetaboliteVirus ProteaseMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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