1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Autophagy
  2. Dopamine Receptor Cytochrome P450 Autophagy 5-HT Receptor
  3. Chlorpromazine

Chlorpromazine  (Synonyms: 氯丙嗪)

目录号: HY-12708 纯度: 99.61%
COA 产品使用指南

Chlorpromazine 是一种口服有效的、可透过血脑屏障的抗精神病剂,能有效拮抗 D2 多巴胺受体和 5-HT2A,已广泛用于精神分裂症和其他精神疾病。Chlorpromazine 可通过多种途径发挥抗癌活性,包括抗增殖、诱导自噬和周期停滞 (G2-M 期)、抑制细胞色素 c 氧化酶 (CcO)、抑制肿瘤生长和转移以及抑制肿瘤免疫逃逸等。Chlorpromazine 还能阻断 hNav1.7 通道 (IC50=25.9 μM; 浓度依赖的方式) 和 HERG 钾通道 (IC50=21.6 μM) ,其在止痛以及心律失常方面也具有较好的研究潜力。Chlorpromazine 也能抑制网格蛋白介导的内吞作用。

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Chlorpromazine Chemical Structure

Chlorpromazine Chemical Structure

CAS No. : 50-53-3

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10 mM * 1 mL in DMSO ¥256
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5 mg ¥233
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10 mg ¥350
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25 mg ¥650
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50 mg ¥980
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Customer Review

Other Forms of Chlorpromazine:

MCE 顾客使用本产品发表的 61 篇科研文献

IF

    Chlorpromazine purchased from MCE. Usage Cited in: Commun Biol. 2022 Nov 14;5(1):1248.  [Abstract]

    Chlorpromazine (CPZ) (10 µM; 30 min) remarkably decreases the cellular internalization of FITC-P-LPK in HCT116 cells. Chlorpromazine can inhibit clathrin-mediated endocytosis. The fluorescence intensity is observed by confocal microscopy and detected using a multi-well plate reader.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Chlorpromazine is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine also can inhibit clathrin-mediated endocytosis[1][2][3][4][5].

    IC50 & Target

    D2 dopamine receptors; 5-HT2A[1][6].

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO IC50
    3.4 μM
    Compound: chlorpromazine
    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-K1 IC50
    1 nM
    Compound: Chlorpromazine
    Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method
    Antagonist activity at human dopamine D2 receptor expressed in CHOK1 cells assessed as inhibition of apomorphine-induced calcium mobilization by radiometric and luminescence plate counting method
    [PMID: 25557493]
    CHO-K1 IC50
    1 nM
    Compound: Chlorpromazine
    Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
    Antagonist activity against human recombinant dopmaine D2L receptor expressed in CHOK1 cells assessed as reduction in apomorphine-induced increase in intracellular Ca2+ levels by aequorin based radiometric and luminescence plate counting method
    [PMID: 25557493]
    Cortical neurone IC50
    13.8 μM
    Compound: Chlorpromazine
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite total length per neuron incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite total length per neuron incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    [PMID: 31841637]
    Cortical neurone IC50
    7.99 μM
    Compound: Chlorpromazine
    Neurotoxicity in rat cortical neuron assessed as inhibition of valid neuron count incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    Neurotoxicity in rat cortical neuron assessed as inhibition of valid neuron count incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    [PMID: 31841637]
    Cortical neurone IC50
    9.022 μM
    Compound: Chlorpromazine
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite outgrowth by measuring mean neurite average length incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    Neurotoxicity in rat cortical neuron assessed as inhibition of neurite outgrowth by measuring mean neurite average length incubated for 72 hrs by Hoechst 33342 staining based ArrayScan analysis
    [PMID: 31841637]
    HaCaT IC50
    36.1 μM
    Compound: CPZ
    Phototoxicity in human HaCaT cells assessed as reduction in cell viability preincubated for 60 mins followed by 7.5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    Phototoxicity in human HaCaT cells assessed as reduction in cell viability preincubated for 60 mins followed by 7.5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    [PMID: 29604584]
    HEK293 IC50
    27 μM
    Compound: chlorpromazine
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
    [PMID: 18788725]
    Macrophage cell line CC50
    22.24 μM
    Compound: CPZ
    Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
    Cytotoxicity in human monocyte-derived macrophages assessed as reduction in cell viability incubated for 3 days by alamar blue dye based assay
    [PMID: 28964936]
    NCI-H1650 GI50
    30.3 μM
    Compound: Chlorpromazine
    Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human NCI-H1650 cells assessed as growth inhibition after 48 hrs by MTT assay
    [PMID: 26372073]
    NHDF IC50
    25.5 μM
    Compound: CPZ
    Phototoxicity in human NHDF cells assessed as reduction in cell viability preincubated for 60 mins followed by 5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    Phototoxicity in human NHDF cells assessed as reduction in cell viability preincubated for 60 mins followed by 5 J/cm2 UVA irradiation and measured after 24 hrs by neutral red uptake assay
    [PMID: 29604584]
    Vero IC50
    26.52 μg/mL
    Compound: CPZ
    Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
    Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability incubated for 72 hrs by resazurin assay
    [PMID: 32526553]
    WI-38 CC50
    10.34 μM
    Compound: Chlorpromazine
    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]
    WI-38 EC50
    7.6 μM
    Compound: Chlorpromazine
    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]
    体外研究
    (In Vitro)

    Chlorpromazine(0、10、20、40 μM;0、24、48 小时)以剂量和时间依赖性方式抑制 U-87MG 胶质瘤细胞的生长[2]
    Chlorpromazine(20 μM;0、12、24、48 小时)12 小时后降低 U-87MG 胶质瘤细胞中的细胞周期蛋白 A 和细胞周期蛋白 B1 的水平[2]
    Chlorpromazine (20 μM) 可抑制细胞周期进程[2]
    Chlorpromazine(10 μM;1 小时)显著抑制 sEV 内化,并显著减少 sEV 处理的骨髓细胞中的 MDSC(MDSC 可显著抑制免疫细胞反应,导致癌细胞免疫抑制)[3]
    Chlorpromazine(3、10、20、40、60 μM)以浓度依赖性方式阻断 hNav1.7 电流[4]
    Chlorpromazine阻断 HERG 钾通道,IC50 值为 21.6 μM,Hill 系数为 1.11[5]

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

    Cell Proliferation Assay[2]

    Cell Line: U-87MG glioma cells
    Concentration: 0, 10, 20, 40 μM
    Incubation Time: 0, 24, 48 h
    Result: Showed anti-proliferative activity in a dose- and time-dependent manner.

    Immunofluorescence[3]

    Cell Line: Bone marrow cells (sEV-treated)
    Concentration: 10 µM
    Incubation Time: 1 h
    Result: Reduced MDSCs and suppressed the sEV internalization.

    Western Blot Analysis[2]

    Cell Line: U-87MG glioma cells
    Concentration: 20 μM
    Incubation Time: 0, 12, 24, 48 h
    Result: Decreased the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged.
    体内研究
    (In Vivo)

    Chlorpromazine(20 mg/kg;腹腔注射;每天一次,连续7天)可抑制裸鼠异种移植肿瘤的生长[2]

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

    Animal Model: 5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors[2].
    Dosage: 20 mg/kg
    Administration: Injected intraperitoneally; single daily for 7 days
    Result: Inhibited tumor growth on day 17.
    分子量

    318.86

    Formula

    C17H19ClN2S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    氯丙嗪

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light, stored under nitrogen

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

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (313.62 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 3.1362 mL 15.6809 mL 31.3617 mL
    5 mM 0.6272 mL 3.1362 mL 6.2723 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, 6 months; -20°C, 1 month (protect from light, 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。

    • 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 (7.84 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 (7.84 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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)。

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

    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: 99.61%

    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, 6 months; -20°C, 1 month (protect from light, 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。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1362 mL 15.6809 mL 31.3617 mL 78.4043 mL
    5 mM 0.6272 mL 3.1362 mL 6.2723 mL 15.6809 mL
    10 mM 0.3136 mL 1.5681 mL 3.1362 mL 7.8404 mL
    15 mM 0.2091 mL 1.0454 mL 2.0908 mL 5.2270 mL
    20 mM 0.1568 mL 0.7840 mL 1.5681 mL 3.9202 mL
    25 mM 0.1254 mL 0.6272 mL 1.2545 mL 3.1362 mL
    30 mM 0.1045 mL 0.5227 mL 1.0454 mL 2.6135 mL
    40 mM 0.0784 mL 0.3920 mL 0.7840 mL 1.9601 mL
    50 mM 0.0627 mL 0.3136 mL 0.6272 mL 1.5681 mL
    60 mM 0.0523 mL 0.2613 mL 0.5227 mL 1.3067 mL
    80 mM 0.0392 mL 0.1960 mL 0.3920 mL 0.9801 mL
    100 mM 0.0314 mL 0.1568 mL 0.3136 mL 0.7840 mL
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    产品名称:
    Chlorpromazine
    目录号:
    HY-12708
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