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

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

目錄號: HY-N0144 純度: 98.88%
COA 產(chǎn)品使用指南 技術(shù)支持

Piperine 是能夠從胡椒中分離的天然生物堿，可以抑制 P-glycoprotein 和 CYP3A4的活性。Piperine 對 HeLa 細(xì)胞的 IC50 為 61.94±0.054 μg/mL。

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

Piperine Chemical Structure

Piperine Chemical Structure

CAS No. : 94-62-2

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥330
In-stock
5 g ￥300
In-stock
10 g ￥500
In-stock
50 g   詢價  

* Please select Quantity before adding items.

Customer Review

Other Forms of Piperine:

    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.

    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.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC50 of 61.94±0.054 μg/mL[1][2][3].

    IC50 & Target

    IC50: 61.94±0.054 μg/mL (P-glycoprotein, HeLa cell)[1]
    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    11.89 μM
    Compound: Piperine
    Antiproliferative activity in human A549 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    Antiproliferative activity in human A549 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    		[PMID: 30108756]
    Bel-7402 IC50
    > 10 μM
    Compound: Piperine
    Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 33026807]
    BTI-TN-5B1-4 IC50
    1.05 μM
    Compound: 1
    Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
    Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho
    		[PMID: 31711793]
    COLO 205 IC50
    46 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) COLO205 cells by SRB assay
    Cytotoxicity against Homo sapiens (human) COLO205 cells by SRB assay
    		10.1007/s00044-010-9500-5
    DLD-1 IC50
    < 200 μM
    Compound: 58
    Anticancer activity against human DLD-1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Anticancer activity against human DLD-1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    		[PMID: 33445154]
    DU-145 IC50
    > 50 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) DU145 cells by SRB assay
    Cytotoxicity against Homo sapiens (human) DU145 cells by SRB assay
    		10.1007/s00044-010-9500-5
    HCT-116 IC50
    < 200 μM
    Compound: 58
    Anticancer activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Anticancer activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    		[PMID: 33445154]
    HeLa IC50
    0.95 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) HeLa cells after 48 hr by MTT assay
    Cytotoxicity against Homo sapiens (human) HeLa cells after 48 hr by MTT assay
    		10.1007/s00044-013-0541-4
    HeLa IC50
    19.21 μM
    Compound: Piperine
    Antiproliferative activity in human HeLa cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    Antiproliferative activity in human HeLa cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    		[PMID: 30108756]
    HEp-2 IC50
    70 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) Hep2 cells by SRB assay
    Cytotoxicity against Homo sapiens (human) Hep2 cells by SRB assay
    		10.1007/s00044-010-9500-5
    Hepatocyte IC50
    12 μM
    Compound: 10
    Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine/TNFalpha-induced cytotoxicity after 20 hrs by MTT assay relative to untreated control
    Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine/TNFalpha-induced cytotoxicity after 20 hrs by MTT assay relative to untreated control
    		[PMID: 19775895]
    HepG2 IC50
    > 10 μM
    Compound: Piperine
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 33026807]
    HUVEC IC50
    100 μM
    Compound: Piperine
    Antiinflammatory activity in HUVEC assessed as inhibition of TNFalpha-induced ICAM-1 expression incubated for 2 hrs prior to TNFalpha challenge measured after 16 hrs by ELISA
    Antiinflammatory activity in HUVEC assessed as inhibition of TNFalpha-induced ICAM-1 expression incubated for 2 hrs prior to TNFalpha challenge measured after 16 hrs by ELISA
    		10.1039/C2MD20216F
    IMR-32 IC50
    10.19 μM
    Compound: Piperine
    Antiproliferative activity in human IMR32 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    Antiproliferative activity in human IMR32 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    		[PMID: 30108756]
    IMR-32 IC50
    89 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) IMR32 cells by SRB assay
    Cytotoxicity against Homo sapiens (human) IMR32 cells by SRB assay
    		10.1007/s00044-010-9500-5
    L929 IC50
    42 μM
    Compound: 10
    Cytoprotective activity in mouse L929 cells assessed as inhibition of TNF-alpha-induced cytotoxicity by MTT assay relative to untreated control
    Cytoprotective activity in mouse L929 cells assessed as inhibition of TNF-alpha-induced cytotoxicity by MTT assay relative to untreated control
    		[PMID: 19775895]
    MCF7 IC50
    0.99 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by MTT assay
    Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by MTT assay
    		10.1007/s00044-013-0541-4
    MCF7 IC50
    12.96 μM
    Compound: Piperine
    Antiproliferative activity in human MCF7 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    Antiproliferative activity in human MCF7 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay
    		[PMID: 30108756]
    MCF7 IC50
    99 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) MCF7 cells by SRB assay
    Cytotoxicity against Homo sapiens (human) MCF7 cells by SRB assay
    		10.1007/s00044-010-9500-5
    MDA-MB-231 IC50
    58.45 μg/mL
    Compound: 3
    Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells assessed as growth inhibition by MTT assay
    		10.1007/s00044-012-0397-z
    Oocyte EC50
    52 μM
    Compound: 5
    Activation of rat GABA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as potentiation of GABA-induced chloride current after 90 secs by two microplate electrode voltage clamp assay
    Activation of rat GABA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as potentiation of GABA-induced chloride current after 90 secs by two microplate electrode voltage clamp assay
    		[PMID: 20085307]
    PC-3 IC50
    > 50 μM
    Compound: 1
    Cytotoxicity against Homo sapiens (human) PC3 cells by SRB assay
    Cytotoxicity against Homo sapiens (human) PC3 cells by SRB assay
    		10.1007/s00044-010-9500-5
    SW480 IC50
    < 200 μM
    Compound: 58
    Anticancer activity against human SW480 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Anticancer activity against human SW480 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    		[PMID: 33445154]
    體外研究
    (In Vitro)

    Piperine 已顯示具有體外 細(xì)胞毒活性和計(jì)算機(jī)研究。IC50 值為 61.94 μg/mL，在計(jì)算機(jī)研究中，它具有更多的氫鍵，具有最小的結(jié)合和對接能量，可被視為 EGFR 酪氨酸激酶抑制劑[1]。已發(fā)現(xiàn) Piperine 具有免疫調(diào)節(jié)、抗氧化、抗哮喘、抗癌、抗炎、抗?jié)兒涂拱⒚装吞匦?sup>[2]。Piperine 可通過抑制 CYP3A 和 P-糖蛋白活性來提高瑞舒伐他汀、紫杉醇和多西紫杉醇 (DOX) 等其他藥物的生物利用度[3]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    在 3.5 mg/kg 的劑量下，Piperine 的生物利用度為 25.36%。其 AUC0→t 隨劑量不成比例地增加，表明 Piperine 具有潛在的非線性藥代動力學(xué)特征。發(fā)現(xiàn) Docetaxel (HY-B0011) 的 AUC0→t 和 C0，與 Piperine 的 t1/2，在聯(lián)合使用后均顯著升高。說明聯(lián)合使用不僅提升了 Docetaxel 的生物利用度，還提升了 Piperine 的生物利用度，這可能會導(dǎo)致藥理作用整體增強(qiáng)[3]。I-κB、p65、p38、ERK 和 JNK 的磷酸化被 Piperine 以劑量依賴的方式抑制，表明 Piperine 可能是子宮內(nèi)膜炎和其他金黃色葡萄球菌引起的疾病中潛在的抗炎藥[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 號
    性狀

    固體

    顏色

    White to light yellow

    中文名稱

    胡椒堿；胡椒酰胺
    結(jié)構(gòu)分類
    初始來源
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 50 mg/mL (175.23 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

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

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?jiān)?年內(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

    動物實(shí)驗(yàn)：

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

    以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請依序添加每種溶劑： 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

      請依序添加每種溶劑： 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。
    動物溶解方案計(jì)算器
    請輸入動物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動物的平均體重

    g

    每只動物的給藥體積

    μL

    動物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動物的量
    請輸入您的動物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動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 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
    動物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
    請確保第一步儲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: 98.88%

    參考文獻(xiàn)
    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.
    參考文獻(xiàn)

    完整儲備液配制表

    * 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請?jiān)?年內(nèi)使用， -20°C儲存時，請?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
    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
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    Inquiry Information

    產(chǎn)品名稱：
    Piperine
    目錄號：
    HY-N0144
    需求量：