1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor
  3. Clozapine

Clozapine  (Synonyms: 氯氮平; HF 1854)

目录号: HY-14539 纯度: 99.97%
COA 产品使用指南

Clozapine (HF 1854) 是用于研究精神分裂症的抗精神病药。Clozapine 对许多神经受体有高度的亲和力,是多巴胺受体的有效拮抗剂,Ki 值为 75 nM。Clozapine 抑制毒蕈碱 M1 受体和血清素 5HT2A 受体,Ki 值分别为 9.5 nM 和 4 nM。Clozapine 也是选择性的毒蕈碱 M4 受体的激动剂 (EC50=11 nM)。

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Clozapine Chemical Structure

Clozapine Chemical Structure

CAS No. : 5786-21-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥880
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50 mg ¥800
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100 mg ¥1220
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Customer Review

Other Forms of Clozapine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].

IC50 & Target[1][4]

5-HT2A Receptor

4 nM (Ki, Inhibitor)

5-HT6 Receptor

 

5-HT7 Receptor

 

mAChR1

9.5 nM (Ki, Antagonist)

mAChR4

11 nM (EC50, Agonist)

α2-adrenergic receptor

51 nM (Ki, Inhibitor)

D2 Receptor

75 nM (Ki, Antagonist)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO IC50
206 nM
Compound: 1
Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay
Inhibition of human dopamine D2L receptor expressed in intact CHO FlpIn cells assessed as inhibition of receptor-mediated mediated ERK1/2 phosphorylation by Alpha-Screen plate-based assay
[PMID: 22243698]
CHO IC50
3.6 μM
Compound: clozapine
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
CHO IC50
4.1 x 10-2 μM
Compound: Clozapine
Displacement of [3H]methyl-spiperone from human recombinant dopamine D4.4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]methyl-spiperone from human recombinant dopamine D4.4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO EC50
56 μM
Compound: clozapine
Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
[PMID: 17870534]
HEK293 IC50
650 nM
Compound: Clozapine
Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay
Inhibition of human ERG expressed in HEK293 cells by electrophysiology assay
[PMID: 23675993]
WI-38 EC50
23.26 μM
Compound: Clozapine
Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
Antiviral activity against BKV Gardner ATCC VR837 infected in human WI38 cells assessed as reduction in viral DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
[PMID: 17893158]
WI-38 CC50
40 μM
Compound: Clozapine
Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
Cytotoxicity against human WI38 cells assessed as reduction in cellular DNA level preincubated for 2 hrs before viral infection measured after 7 days by real time PCR assay
[PMID: 17893158]
体外研究
(In Vitro)

Clozapine (HF 1854) 是一种 D2 受体拮抗剂,Ki 为 75 nM,阻断血清素 5HT2A 受体,Ki 为 4 nM,抑制毒蕈碱 M1 受体Ki 为 9.5 nM,阻断 α2-肾上腺素受体,Ki 值为 51 nM[1]
Clozapine (0-1 μM;24 h) 在 HeLa 细胞中下调 5-HT6 并上调 5-HT7 受体[2]
Clozapine 是 CHO 细胞中表达的毒蕈碱 M4 受体 (EC50=11 nM) 的完全激动剂[4]

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

体内研究
(In Vivo)

Clozapine (HF 1854) (25 mg/kg/天;腹腔注射;21 天) 在麦角酸二乙胺诱导的精神病小鼠模型中显示出抗精神病作用[3]

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

Animal Model: Male 129 S6/Sv mice, lysergic acid diethylamide (LSD)-induced psychosis model[3]
Dosage: 25 mg/kg/day
Administration: Intraperitoneal injection, 21 days
Result: Decreased head-twitch response, reduced 5-HT2A mRNA, rescued induction of c-fos, but not egr-1 and egr-2.
Clinical Trial
分子量

326.82

Formula

C18H19ClN4

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

氯氮平

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 1 year
-20°C 6 months
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (152.99 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.0598 mL 15.2989 mL 30.5979 mL
5 mM 0.6120 mL 3.0598 mL 6.1196 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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

  • 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 (7.65 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。

    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 (7.65 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。

    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

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
参考文献

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, 1 year; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0598 mL 15.2989 mL 30.5979 mL 76.4947 mL
5 mM 0.6120 mL 3.0598 mL 6.1196 mL 15.2989 mL
10 mM 0.3060 mL 1.5299 mL 3.0598 mL 7.6495 mL
15 mM 0.2040 mL 1.0199 mL 2.0399 mL 5.0996 mL
20 mM 0.1530 mL 0.7649 mL 1.5299 mL 3.8247 mL
25 mM 0.1224 mL 0.6120 mL 1.2239 mL 3.0598 mL
30 mM 0.1020 mL 0.5100 mL 1.0199 mL 2.5498 mL
40 mM 0.0765 mL 0.3825 mL 0.7649 mL 1.9124 mL
50 mM 0.0612 mL 0.3060 mL 0.6120 mL 1.5299 mL
60 mM 0.0510 mL 0.2550 mL 0.5100 mL 1.2749 mL
80 mM 0.0382 mL 0.1912 mL 0.3825 mL 0.9562 mL
100 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7649 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.

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Clozapine
目录号:
HY-14539
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