1. Membrane Transporter/Ion Channel Autophagy Metabolic Enzyme/Protease
  2. P-glycoprotein Autophagy Endogenous Metabolite
  3. Piperine

Piperine  (Synonyms: 胡椒碱; Bioperine; 1-Piperoylpiperidine)

目录号: HY-N0144 纯度: 98.88%
COA 产品使用指南

Piperine是从胡椒中分离的天然生物碱,可以抑制P-glycoprotein and CYP3A4的活性,在HeLa细胞中的IC50值为61.94±0.054 μg/mL。

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Piperine Chemical Structure

Piperine Chemical Structure

CAS No. : 94-62-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥330
In-stock
5 g ¥300
In-stock
10 g ¥500
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50 g   询价  

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Top Publications Citing Use of Products

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine targets NLRP3 inflammasome in HK-2 cells. The protein levels of indicated proteins in cell lysates and from culture medium are examined by Western blot.

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine targets NLRP3 inflammasome by blocking AMPK activation. HK-2 cells are treated as indicated.

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine inhibits the activation of NLRP3 inflammasome. The protein levels of indicated targets are examined by Western blot.

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine inhibits AMPK activation. HK-2 cells are treated as indicated and the levels of p-AMPK, total AMPK, and β-tubulin are examined by Western blot.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/mL in HeLa cell.

    IC50 & Target

    IC50: 61.94±0.054 μg/mL (P-glycoprotein, HeLa cell)[1]

    体外研究
    (In Vitro)

    Piperine 已显示具有体外 细胞毒活性和计算机研究。IC50 值为 61.94 μg/mL,在计算机研究中,它具有更多的氢键,具有最小的结合和对接能量,可被视为 EGFR 酪氨酸激酶抑制剂[1]。已发现 Piperine 具有免疫调节、抗氧化、抗哮喘、抗癌、抗炎、抗溃疡和抗阿米巴特性[2]。Piperine 可通过抑制 CYP3A 和 P-糖蛋白活性来提高瑞舒伐他汀、紫杉醇和多西紫杉醇 (DOX) 等其他药物的生物利用度[3]

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

    体内研究
    (In Vivo)

    在 3.5 mg/kg 的剂量下,Piperine 的生物利用度为 25.36%。其 AUC0→t 随剂量不成比例地增加,表明 Piperine 具有潜在的非线性药代动力学特征。发现 Docetaxel (HY-B0011) 的 AUC0→t 和 C0,与 Piperine 的 t1/2,在联合使用后均显著升高。说明联合使用不仅提升了 Docetaxel 的生物利用度,还提升了 Piperine 的生物利用度,这可能会导致药理作用整体增强[3]。I-κB、p65、p38、ERK 和 JNK 的磷酸化被 Piperine 以剂量依赖的方式抑制,表明 Piperine 可能是子宫内膜炎和其他金黄色葡萄球菌引起的疾病中潜在的抗炎药[4]

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

    Clinical Trial
    分子量

    285.34

    Formula

    C17H19NO3

    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    胡椒碱;胡椒酰胺

    结构分类
    初始来源
    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 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (175.23 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 3.5046 mL 17.5230 mL 35.0459 mL
    5 mM 0.7009 mL 3.5046 mL 7.0092 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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

    In Vivo:

    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 (8.76 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 (8.76 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。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):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

    纯度: 98.88%

    参考文献
    Cell Assay
    [1]

    Standard solution is prepared by dissolving 10 mg of piperine in 100 mL of methanol. The MTT assay is carried out to measure cell viability. Ten thousand cells in 100 μL of DMEM media are seeded in the wells of a 96-well plate. After 24 h, existing media is removed and 100 μL of various concentrations of piperine (20–100 μg/mL) are added and incubated for 48 h at 37 °C in a CO2 incubator. Control cells are supplemented with 0.05 % DMSO vehicle. At the 48th hour of incubation, MTT (10 μL of 5 mg/mL) is added to the plate. The contents of the plate are pipetted out carefully, the formazan crystals formed are dissolved in 100 μL of DMSO, and the absorbance is measured at 550 nm in a microplate reader[1].

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

    Animal Administration
    [3][4]

    Rats: The stock solutions of piperine (PIP) and docetaxel (DOX)are prepared by dissolving appropriate amount of each authentic compound in DMSO separately at 1 mg/mL. The standard solutions containing both PIP and DOX are prepared by serial dilution of the stock solutions with 0.2% formic acid and acetonitrile (50:50, v/v) to yield concentrations of 25, 50, 100, 200, 400, 800, 1600, 3200, 6400, 12800 ng/mL. 25 Sprague-Dawley rats are divided into five groups receiving DOX(Group DOX 7 iv, 7 mg/kg, i.v.), PIP (Group PIP 35 po, 35 mg/kg,p.o.) and their combined administration (Group DOX+PIP) as well as PIP (Group PIP 3.5 po, 3.5 mg/kg, p.o.) and PIP (Group PIP 3.5 iv, 3.5 mg/kg, i.v.)[3].

    Mice: Piperine is dissolved in 5 mL of tris buffered saline (TBS) at concentrations corresponding to 25, 50, and 100 mg/kg, based on the weight of the mice. After 24 h of S. aureus infection in the uterus, the piperine solution is injected intraperitoneally three times every 6 h. A total of 60 female BALB/c mice are used in this study. All mice are maintained on a 12 h light/dark cycle and cafeteria feeding[4].

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

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.5046 mL 17.5230 mL 35.0459 mL 87.6148 mL
    5 mM 0.7009 mL 3.5046 mL 7.0092 mL 17.5230 mL
    10 mM 0.3505 mL 1.7523 mL 3.5046 mL 8.7615 mL
    15 mM 0.2336 mL 1.1682 mL 2.3364 mL 5.8410 mL
    20 mM 0.1752 mL 0.8761 mL 1.7523 mL 4.3807 mL
    25 mM 0.1402 mL 0.7009 mL 1.4018 mL 3.5046 mL
    30 mM 0.1168 mL 0.5841 mL 1.1682 mL 2.9205 mL
    40 mM 0.0876 mL 0.4381 mL 0.8761 mL 2.1904 mL
    50 mM 0.0701 mL 0.3505 mL 0.7009 mL 1.7523 mL
    60 mM 0.0584 mL 0.2920 mL 0.5841 mL 1.4602 mL
    80 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
    100 mM 0.0350 mL 0.1752 mL 0.3505 mL 0.8761 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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