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  1. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Membrane Transporter/Ion Channel Apoptosis
  2. PDHK Reactive Oxygen Species NKCC Apoptosis
  3. Sodium dichloroacetate

Sodium dichloroacetate  (Synonyms: 二氯乙酸鈉)

目錄號(hào): HY-Y0445A 純度: 99.76%
COA 產(chǎn)品使用指南

Sodium dichloroacetate 是癌細(xì)胞線粒體中的一種代謝調(diào)節(jié)劑,具有抗癌活性。Sodium dichloroacetate 抑制丙酮酸脫氫酶激酶 (PDHK),從而導(dǎo)致腫瘤微環(huán)境中的乳酸減少。Sodium dichloroacetate 增加活性氧 (ROS) 的產(chǎn)生并促進(jìn)癌細(xì)胞凋亡,還可作為 NKCC 抑制劑。

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Sodium dichloroacetate Chemical Structure

Sodium dichloroacetate Chemical Structure

CAS No. : 2156-56-1

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Customer Review

Other Forms of Sodium dichloroacetate:

    Sodium dichloroacetate purchased from MCE. Usage Cited in: Life Sciences. 2022: 121192.

    Sodium dichloroacetate (DCA; 10 mM; 48 h) significantly inhibits hypoxia-induced proliferation of HPASMCs (Fig I) , and markedly increases the apoptosis rate (Fig J).
    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor[1].

    IC50 & Target

    PDHK; Reactive oxygen species (ROS); Apoptosis; NKCC[1]

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    4T1 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against mouse 4T1 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against mouse 4T1 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    A-375 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against human A375 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against human A375 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    A-375 IC50
    20.1 mM
    Compound: DCA
    Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human A375 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    A549 IC50
    1011 μM
    Compound: DCA
    Anticancer activity against human A549 cells after 72 hrs by MTT assay
    Anticancer activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 20663593]
    A549 IC50
    19.5 mM
    Compound: DCA
    Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    A549 IC50
    20.1 mM
    Compound: DCA
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30470491]
    A549 IC50
    23.58 mM
    Compound: DCA
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27006991]
    A549 IC50
    4286 μM
    Compound: DCA
    Cytotoxicity against human A549 cells after 68 hrs by MTT assay
    Cytotoxicity against human A549 cells after 68 hrs by MTT assay
    [PMID: 23067553]
    Bel-7402 IC50
    860 μM
    Compound: DCA
    Anticancer activity against human Bel7402 cells after 72 hrs by MTT assay
    Anticancer activity against human Bel7402 cells after 72 hrs by MTT assay
    [PMID: 20663593]
    BGC-823 IC50
    1051 μM
    Compound: DCA
    Anticancer activity against human BGC823 cells after 72 hrs by MTT assay
    Anticancer activity against human BGC823 cells after 72 hrs by MTT assay
    [PMID: 20663593]
    HCT-116 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against human HCT116 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against human HCT116 cells expressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    HCT-116 IC50
    9.8 mM
    Compound: DCA
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human HCT-116 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    KB IC50
    1424 μM
    Compound: DCA
    Anticancer activity against human KB cells after 72 hrs by MTT assay
    Anticancer activity against human KB cells after 72 hrs by MTT assay
    [PMID: 20663593]
    KB 3-1 IC50
    5883 μM
    Compound: DCA
    Cytotoxicity against human KB-3-1 cells after 68 hrs by MTT assay
    Cytotoxicity against human KB-3-1 cells after 68 hrs by MTT assay
    [PMID: 23067553]
    L02 IC50
    > 100 μM
    Compound: Na-DCA
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human LO2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    L02 IC50
    21.7 mM
    Compound: DCA
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 33550182]
    MCF7 IC50
    > 100 μM
    Compound: Na-DCA
    Anticancer activity against human MCF7 cells overexpressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    Anticancer activity against human MCF7 cells overexpressing PDK assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 31509699]
    MCF7 IC50
    12.35 mM
    Compound: DCA
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 27006991]
    MCF7 IC50
    13.4 mM
    Compound: DCA
    Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    NCI-H1650 IC50
    16.3 mM
    Compound: DCA
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 30470491]
    NCI-H460 IC50
    3892 μM
    Compound: DCA
    Cytotoxicity against human H460 cells after 68 hrs by MTT assay
    Cytotoxicity against human H460 cells after 68 hrs by MTT assay
    [PMID: 23067553]
    PC-3 IC50
    15.7 mM
    Compound: DCA
    Antiproliferative activity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    SH-SY5Y IC50
    17.4 mM
    Compound: DCA
    Antiproliferative activity against human SHSY-5Y cells assessed as growth inhibition after 72 hrs by MTT assay
    Antiproliferative activity against human SHSY-5Y cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 33550182]
    體外研究
    (In Vitro)

    Sodium dichloroacetate 可增加線粒體中的 ROS 生成。Sodium dichloroacetate 通過(guò)促進(jìn)氧化代謝而增加 ROS 生成,從而影響細(xì)胞生長(zhǎng)和活力。Sodium dichloroacetate 對(duì)多發(fā)性骨髓瘤細(xì)胞活力、細(xì)胞周期停滯和細(xì)胞凋亡的影響與丙酮酸脫氫酶激酶 (PDK) 抑制、丙酮酸脫氫酶 (PDH) 活性恢復(fù)以及促進(jìn)氧化代謝有關(guān),同時(shí)還與細(xì)胞內(nèi) ROS 生成增加有關(guān),而細(xì)胞內(nèi) ROS 生成增加取決于 Sodium dichloroacetate 的劑量。Sodium dichloroacetate 作用與 CI 抑制協(xié)同促進(jìn)大鼠 VM-M3 膠質(zhì)母細(xì)胞瘤細(xì)胞中的氧化應(yīng)激。經(jīng) Sodium dichloroacetate 處理的癌細(xì)胞中 ROS 水平升高與誘導(dǎo)凋亡有關(guān),而凋亡與細(xì)胞色素 c 表達(dá)增加有關(guān)。Sodium dichloroacetate 導(dǎo)致 ROS 依賴性 T 細(xì)胞分化[1]。

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

    體內(nèi)研究
    (In Vivo)

    Sodium dichloroacetate 處理的性腺完整和閹割的雄性大鼠中 NKCC1 RNA 表達(dá)水平顯著降低,而 Sodium dichloroacetate 處理的性腺完整和閹割的雌性大鼠中沒有發(fā)現(xiàn)這種影響[1]。
    單劑量 Sodium dichloroacetate 可顯著增加 Wistar 雄性大鼠的 24 小時(shí)利尿量,而利尿量的增加與 NKCC2 抑制有關(guān)。與完整雄性大鼠相比,完整雌性大鼠腎臟中的 NKCC2 更豐富,Sprague-Dawley 雌性大鼠的轉(zhuǎn)運(yùn)蛋白密度更高[1]
    口服 5、20 和 100 mg/kg Sodium dichloroacetate 在雄性大鼠體內(nèi)的生物利用度顯著低于 GSTζ 缺乏的大鼠(分別為 10%、13%、81% 和 31%、75%、100%)。GSTζ 缺乏的大鼠體內(nèi) Sodium dichloroacetate 的肝臟提取具有線性動(dòng)力學(xué),但在較高劑量下隨著代謝飽和而降低[1]

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

    Clinical Trial
    分子量

    150.92

    Formula

    C2HCl2NaO2

    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    二氯乙酸鈉

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.

    儲(chǔ)存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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

    H2O 中的溶解度 : 100 mg/mL (662.60 mM; 超聲助溶)

    DMSO 中的溶解度 : 25 mg/mL (165.65 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響,請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 6.6260 mL 33.1301 mL 66.2603 mL
    5 mM 1.3252 mL 6.6260 mL 13.2521 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 (sealed storage, away from moisture)。-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。

    * 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

    • 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):

    以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 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: PBS

      Solubility: 100 mg/mL (662.60 mM); 澄清溶液; 超聲助溶

    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
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    該產(chǎn)品水溶性佳,請(qǐng)具體參考實(shí)測(cè) 水 / PBS / Saline 中的溶解度數(shù)據(jù)。
    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,如有需要,請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    純度 & 產(chǎn)品資料

    純度: 99.76%

    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 (sealed storage, away from moisture)。-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 / H2O 1 mM 6.6260 mL 33.1301 mL 66.2603 mL 165.6507 mL
    5 mM 1.3252 mL 6.6260 mL 13.2521 mL 33.1301 mL
    10 mM 0.6626 mL 3.3130 mL 6.6260 mL 16.5651 mL
    15 mM 0.4417 mL 2.2087 mL 4.4174 mL 11.0434 mL
    20 mM 0.3313 mL 1.6565 mL 3.3130 mL 8.2825 mL
    25 mM 0.2650 mL 1.3252 mL 2.6504 mL 6.6260 mL
    30 mM 0.2209 mL 1.1043 mL 2.2087 mL 5.5217 mL
    40 mM 0.1657 mL 0.8283 mL 1.6565 mL 4.1413 mL
    50 mM 0.1325 mL 0.6626 mL 1.3252 mL 3.3130 mL
    60 mM 0.1104 mL 0.5522 mL 1.1043 mL 2.7608 mL
    80 mM 0.0828 mL 0.4141 mL 0.8283 mL 2.0706 mL
    100 mM 0.0663 mL 0.3313 mL 0.6626 mL 1.6565 mL

    * 備注:如您選擇水作為儲(chǔ)備液,請(qǐng)稀釋至工作液后,再用 0.22 μm 的濾膜過(guò)濾除菌后使用。

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    產(chǎn)品名稱:
    Sodium dichloroacetate
    目錄號(hào):
    HY-Y0445A
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