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  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)

目錄號(hào): HY-12708 純度: 99.61%
COA 產(chǎn)品使用指南

Chlorpromazine 是一種口服有效的、可透過(guò)血腦屏障的抗精神病劑,能有效拮抗 D2 多巴胺受體和 5-HT2A,已廣泛用于精神分裂癥和其他精神疾病。Chlorpromazine 可通過(guò)多種途徑發(fā)揮抗癌活性,包括抗增殖、誘導(dǎo)自噬和周期停滯 (G2-M 期)、抑制細(xì)胞色素 c 氧化酶 (CcO)、抑制腫瘤生長(zhǎng)和轉(zhuǎn)移以及抑制腫瘤免疫逃逸等。Chlorpromazine 還能阻斷 hNav1.7 通道 (IC50=25.9 μM; 濃度依賴的方式) 和 HERG 鉀通道 (IC50=21.6 μM) ,其在止痛以及心律失常方面也具有較好的研究潛力。Chlorpromazine 也能抑制網(wǎng)格蛋白介導(dǎo)的內(nèi)吞作用。

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Chlorpromazine Chemical Structure

Chlorpromazine Chemical Structure

CAS No. : 50-53-3

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Customer Review

Other Forms of Chlorpromazine:

MCE 顧客使用本產(chǎn)品發(fā)表的 61 篇科研文獻(xiàn)

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

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    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].

    細(xì)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]
    體外研究
    (In Vitro)

    Chlorpromazine(0、10、20、40 μM;0、24、48 小時(shí))以劑量和時(shí)間依賴性方式抑制 U-87MG 膠質(zhì)瘤細(xì)胞的生長(zhǎng)[2]。
    Chlorpromazine(20 μM;0、12、24、48 小時(shí))12 小時(shí)后降低 U-87MG 膠質(zhì)瘤細(xì)胞中的細(xì)胞周期蛋白 A 和細(xì)胞周期蛋白 B1 的水平[2]。
    Chlorpromazine (20 μM) 可抑制細(xì)胞周期進(jìn)程[2]。
    Chlorpromazine(10 μM;1 小時(shí))顯著抑制 sEV 內(nèi)化,并顯著減少 sEV 處理的骨髓細(xì)胞中的 MDSC(MDSC 可顯著抑制免疫細(xì)胞反應(yīng),導(dǎo)致癌細(xì)胞免疫抑制)[3]。
    Chlorpromazine(3、10、20、40、60 μM)以濃度依賴性方式阻斷 hNav1.7 電流[4]。
    Chlorpromazine阻斷 HERG 鉀通道,IC50 值為 21.6 μM,Hill 系數(shù)為 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.
    體內(nèi)研究
    (In Vivo)

    Chlorpromazine(20 mg/kg;腹腔注射;每天一次,連續(xù)7天)可抑制裸鼠異種移植腫瘤的生長(zhǎng)[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 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    氯丙嗪

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)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)

    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn): 

    DMSO 中的溶解度 : 100 mg/mL (313.62 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開(kāi)封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)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
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備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儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

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

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn):

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液,再依次添加助溶劑:
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)天使用;
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (7.84 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL(飽和度未知)的澄清溶液。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (7.84 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液,懸濁液可用于口服和腹腔注射。

      1 mL 工作液為例,取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中,混合均勻。

      2 g SBE-β-CD(磺丁基醚 β-環(huán)糊精)粉末定容于 10 mL 的生理鹽水中,完全溶解至澄清透明。
    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    由于實(shí)驗(yàn)過(guò)程有損耗,建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠,建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。
    方案所需 助溶劑 包括:DMSO ,均可在 MCE 網(wǎng)站選購(gòu)。 Tween 80,均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO(母液濃度為 mg/mL)。

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

    您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度,以下方案僅供參考,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液,加入 μL 。 μL ,混合均勻至澄清,再加 μL Tween 80,混合均勻至澄清,再加 μL 生理鹽水
    連續(xù)給藥周期超過(guò)半月以上,請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài),從左到右依次添加助溶劑。您可采用超聲加熱 (超聲清洗儀,建議頻次 20-40 kHz),渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.61%

    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備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儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)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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    產(chǎn)品名稱:
    Chlorpromazine
    目錄號(hào):
    HY-12708
    需求量: