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  2. Cell Cycle/DNA Damage Epigenetics Autophagy Anti-infection Stem Cell/Wnt Neuronal Signaling Apoptosis Metabolic Enzyme/Protease
  3. Organoid HDAC Autophagy Mitophagy HIV Notch Apoptosis Endogenous Metabolite
  4. Valproic acid

Valproic acid  (Synonyms: 丙戊酸; Dipropylacetic Acid)

目錄號(hào): HY-10585 純度: 99.19%
COA 產(chǎn)品使用指南 技術(shù)支持

Valproic acid (VPA) 是一種具有口服活性的 HDAC 抑制劑，IC50 值為 0.5-2 mM。 Valproic acid 抑制 HDAC1 的活性，(IC50，400 μM)，同時(shí)可誘導(dǎo) HDAC2 的降解。Valproic acid 激活 Notch1 信號(hào)并抑制小細(xì)胞肺癌 (SCLC) 細(xì)胞的增殖。Valproic acid 可用于癲癇、雙相情感障礙、代謝疾病、HIV 感染和偏頭痛等的研究。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

Valproic acid Chemical Structure

Valproic acid Chemical Structure

CAS No. : 99-66-1

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規(guī)格 價(jià)格 是否有貨 數(shù)量
500 mg ￥350
In-stock
1 g ￥450
In-stock
5 g ￥800
In-stock
25 g ￥1000
In-stock
50 g   詢價(jià)  

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Customer Review

Other Forms of Valproic acid:

MCE 顧客使用本產(chǎn)品發(fā)表的 41 篇科研文獻(xiàn)

WB

    Valproic acid purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2020 Jun 17.  [Abstract]

    Effects of Butyrate (But, 1 mM), Vpa (5 mM) and SAHA (Vor, 1 μM) on the expression of P-gp and BCRP, NF-кB p65 and phosphorylated p65 (p-p65), and IкBα and phosphorylated IкBα (p-IкBα).

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7].

    IC50 & Target[5][6]

    HDAC1

    400 μM (IC50)

    HDAC

    0.5-2 mM (IC50)

    HDAC2

     

    Autophagy

     

    Mitophagy

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A498 IC50
    2141.25 μM
    Compound: VPA
    Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
    Antiproliferative activity against human A498 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
    		[PMID: 34111829]
    A549 IC50
    > 1000 nM
    Compound: VPA
    Antiproliferative activity against human A549 cells after 3 days
    Antiproliferative activity against human A549 cells after 3 days
    		[PMID: 18294844]
    Caco-2 IC50
    > 1000 μM
    Compound: VPA
    Growth inhibition of human Caco2 cells after 48 hrs by MTT assay
    Growth inhibition of human Caco2 cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    CAKI-1 IC50
    2825.37 μM
    Compound: VPA
    Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
    Antiproliferative activity against human CAKI-1 cells assessed as cell growth inhibition incubated for 24 hrs by MTT assay
    		[PMID: 34111829]
    HeLa IC50
    1000 μM
    Compound: VPA
    Growth inhibition of human HeLa cells after 48 hrs by MTT assay
    Growth inhibition of human HeLa cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    HeLa IC50
    7.24 mM
    Compound: Valproic acid
    Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay
    Inhibition of HDAC in human Hela cells nuclear extracts by fluorimetric assay
    		[PMID: 19520580]
    Hepatocyte EC50
    11.73 μM
    Compound: 4
    Reduction of propionyl-CoA in human hepatocytes derived from propionic acidemia patient pretreated for 30 mins followed by 13C-isoleucine addition and measured after 1 hr by MS/MS analysis
    Reduction of propionyl-CoA in human hepatocytes derived from propionic acidemia patient pretreated for 30 mins followed by 13C-isoleucine addition and measured after 1 hr by MS/MS analysis
    		[PMID: 33848153]
    HL-60 IC50
    1.7 mM
    Compound: VPA
    Cytotoxicity against human HL60 cells after 24 to 48 hrs by trypan blue dye exclusion method
    Cytotoxicity against human HL60 cells after 24 to 48 hrs by trypan blue dye exclusion method
    		[PMID: 25304896]
    HL-60 IC50
    1700 μM
    Compound: VPA
    Growth inhibition of human HL60 cells after 48 hrs by MTT assay
    Growth inhibition of human HL60 cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    HT-29 IC50
    > 1000 μM
    Compound: VPA
    Growth inhibition of human HT-29 cells after 48 hrs by MTT assay
    Growth inhibition of human HT-29 cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    HuT78 IC50
    1800 μM
    Compound: VPA
    Growth inhibition of human HUT78 cells after 48 hrs by MTT assay
    Growth inhibition of human HUT78 cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    HUVEC IC50
    1.5 mM
    Compound: valproic acid
    Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay
    Inhibition of LPS-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of LPS challenge by one stage clotting assay
    		[PMID: 17675290]
    HUVEC IC50
    2 mM
    Compound: valproic acid
    Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay
    Inhibition of TNF-alpha-induced tissue factor activity in HUVEC preincubated for 4 hrs assessed after 4 hrs of TNFalpha challenge by one stage clotting assay
    		[PMID: 17675290]
    K562 IC50
    > 1000 μM
    Compound: VPA
    Growth inhibition of human K562 cells after 48 hrs by MTT assay
    Growth inhibition of human K562 cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    MCF7 IC50
    230 μM
    Compound: VPA
    Growth inhibition of human MCF7 cells after 48 hrs by MTT assay
    Growth inhibition of human MCF7 cells after 48 hrs by MTT assay
    		[PMID: 25304896]
    體外研究
    (In Vitro)

    Valproic acid (0-15 mM；24 和 72 小時(shí)) 以劑量和時(shí)間依賴性方式抑制 Hela 細(xì)胞生長(zhǎng)[1]。
    Valproic acid（10 mM；24 小時(shí)）顯著減弱總、細(xì)胞質(zhì)和核 HDAC 的活性[1]。
    Valproic acid (0-15 mM；24 小時(shí)) 在 1-3 mM 時(shí)誘導(dǎo) G1 期停滯，在 10 mM 時(shí)誘導(dǎo) G2/M 期停滯，并增加 HeLa 細(xì)胞中亞 G1 細(xì)胞的百分比。Valproic acid 還會(huì)誘導(dǎo)壞死、凋亡和乳酸脫氫酶 (LDH) 釋放[1]。
    Valproic acid (0-20 mM; 24 小時(shí)) 激活 Tcf/Lef 依賴性轉(zhuǎn)錄并與鋰產(chǎn)生協(xié)同作用[2]。
    Valproic acid（0-5 mM；0-18 小時(shí)）可增加 Neuro2A 細(xì)胞中的 β-catenin 水平[2]。
    Valproic acid（0-2 mM；0-24 小時(shí)）刺激肝細(xì)胞中 AMPK 和 ACC 的磷酸化[5]。
    Valproic acid（0-10 mM；2 天）誘導(dǎo) Notch1 信號(hào)傳導(dǎo)和形態(tài)分化，抑制 SCLC 細(xì)胞中 NE 腫瘤標(biāo)志物的產(chǎn)生[6]。

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

    Cell Viability Assay[1]

    Cell Line: HeLa cells
    Concentration: 0, 1, 3, 5, 10 and 15 mM
    Incubation Time: 24 and 72 h
    Result: HeLa cell growth was dose- and time-dependently decreased with an IC50 of ~10 and 4 mM at 24 and 72 h.

    Western Blot Analysis[1][2][5]

    Cell Line: HeLa cells, Neuro2A cells or primary mouse hepatocytes
    Concentration: 10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 mM (hepatocytes)
    Incubation Time: 10 mM (HeLa); 0, 2, and 5 mM (Neuro2A); 0.2, 0.4, 0.8, 1.2 and 2 Mm (hepatocytes)
    Result: Increased the form of acetylated histone 3.
    Reduced PARP, induced cleavage PARP, and downregulated Bcl-2.
    Increased β-catenin levels.
    Increased the phosphorylation of AMPK and ACC.

    Cell Cycle Analysis[1]

    Cell Line: HeLa cells
    Concentration: 0, 1, 3, 5, 10 and 15 mM
    Incubation Time: 24 h
    Result: Induced a G1 phase arrest at 1–3 mM, significantly induced a G2/M phase arrest at 10 mM, and increased the percentage of sub-G1 cells in HeLa cells in a dose-dependent manner at 24 h.
    體內(nèi)研究
    (In Vivo)

    Valproic acid（500 mg/kg；腹腔注射；每天注射 12 天）可抑制移植了 Kasumi-1 細(xì)胞的小鼠的腫瘤血管生成[3]。
    Valproic acid（350 mg/kg；腹腔注射；一次）可增強(qiáng)大鼠的社交行為[4]。
    Valproic acid（0.26% (w/v)；通過(guò)飲用水口服；14 天）可降低肥胖小鼠的肝臟質(zhì)量、肝臟脂肪堆積和血糖，且無(wú)肝毒性[5]。

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

    Animal Model: Female BALB/c nude mice, Kasumi-1 tumor model[3]
    Dosage: 500 mg/kg
    Administration: Intraperitoneal injection, daily for 12 days
    Result: Inhibited tumor growth and tumor angiogenesis.
    Inhibited the mRNA and protein expression of VEGF, VEGFR2 and bFGF.
    Inhibited HDAC activity and increased acetylation of histone H3.
    Enhanced the accumulation of hyperacetylated histone H3 on VEGF promoters.
    Animal Model: Timed-pregnant Long Evans rats[4]
    Dosage: 350 mg/kg
    Administration: Intraperitoneal injection, once
    Result: Demonstrated more social investigation and play fighting than control animals.
    Animal Model: Obese phenotype of ob/ob mice[5]
    Dosage: 0.26% (w/v)
    Administration: Oral via drinking water, 14 days
    Result: Revealed a marked reduction in the accumulation of fats in the liver as compared with the untreated mice, significantly decreased liver mass to body mass, decreased serum triglyceride concentrations, and did not induce hepatotoxicity.
    分子量

    144.21

    Formula

    C8H16O2
    CAS 號(hào)
    性狀

    液體（密度：0.92 g/cm3）

    顏色

    Colorless to light yellow

    中文名稱

    丙戊酸；2-丙基戊酸；二丙基乙酸
    結(jié)構(gòu)分類
    初始來(lái)源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式

    Store at room temperature 3 years

    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 100 mg/mL (693.41 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)

    0.1 M NaOH 中的溶解度 : 5 mg/mL (34.67 mM; 超聲助溶)

    H2O 中的溶解度 : 2.5 mg/mL (17.34 mM; 超聲助溶 (<60°C))

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 6.9341 mL 34.6707 mL 69.3414 mL
    5 mM 1.3868 mL 6.9341 mL 13.8683 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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(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)：

    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 (17.34 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。

      以 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 (17.34 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。

      以 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。

    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: 2 mg/mL (13.87 mM); 澄清溶液; 超聲助溶

    • 方案 二

      請(qǐng)依序添加每種溶劑： 50% PEG300    50% Saline

      Solubility: 25 mg/mL (173.35 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

    只
    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）。
    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: 99.19%

    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, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    H2O / 0.1 M NaOH / DMSO 1 mM 6.9341 mL 34.6707 mL 69.3414 mL 173.3535 mL
    5 mM 1.3868 mL 6.9341 mL 13.8683 mL 34.6707 mL
    10 mM 0.6934 mL 3.4671 mL 6.9341 mL 17.3353 mL
    15 mM 0.4623 mL 2.3114 mL 4.6228 mL 11.5569 mL
    0.1 M NaOH / DMSO 20 mM 0.3467 mL 1.7335 mL 3.4671 mL 8.6677 mL
    25 mM 0.2774 mL 1.3868 mL 2.7737 mL 6.9341 mL
    30 mM 0.2311 mL 1.1557 mL 2.3114 mL 5.7784 mL
    DMSO 40 mM 0.1734 mL 0.8668 mL 1.7335 mL 4.3338 mL
    50 mM 0.1387 mL 0.6934 mL 1.3868 mL 3.4671 mL
    60 mM 0.1156 mL 0.5778 mL 1.1557 mL 2.8892 mL
    80 mM 0.0867 mL 0.4334 mL 0.8668 mL 2.1669 mL
    100 mM 0.0693 mL 0.3467 mL 0.6934 mL 1.7335 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。

    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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