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  2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Apoptosis
  3. PPAR Ferroptosis
  4. Pioglitazone

Pioglitazone  (Synonyms: 吡格列酮; U 72107)

目錄號(hào): HY-13956 純度: 99.89%
COA 產(chǎn)品使用指南

Pioglitazone (U 72107) 是一種具有口服活性的選擇性 PPARγ (peroxisome proliferator-activated receptor) 激動(dòng)劑，高親和力結(jié)合到 PPARγ 配體結(jié)合域，作用于人和鼠 PPARγ 的 EC50 分別為 0.93 和 0.99 μM。Pioglitazone 可用于糖尿病研究。

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)

Pioglitazone Chemical Structure

Pioglitazone Chemical Structure

CAS No. : 111025-46-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥773
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5 mg ￥439
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10 mg ￥703
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50 mg ￥1234
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100 mg ￥1727
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200 mg   詢價(jià)  
500 mg   詢價(jià)  

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Customer Review

Other Forms of Pioglitazone:

MCE 顧客使用本產(chǎn)品發(fā)表的 29 篇科研文獻(xiàn)

WB

    Pioglitazone purchased from MCE. Usage Cited in: Inflammation. 2020 Apr;43(2):568-578.  [Abstract]

    Colonic lysates of CON + Veh, DSS + Veh, and DSS + PIO (day 7, day 14, and day 21) group mice are analyzed by immunoblotting with IL-6, TNF-α, MMP9, and PPARγ antibodies, respectively. Each lane represents one mouse.

    Pioglitazone purchased from MCE. Usage Cited in: Inflammation. 2020 Apr;43(2):568-578.  [Abstract]

    Colonic lysates of CON + Veh, DSS + Veh, and DSS + PIO (day 7, day 14, and day 21) group mice are analyzed by immunoblotting with p-ERK, ERK, p-P65, and P65 antibodies, respectively. Each lane represents one mouse.

    查看 PPAR 亞型特異性產(chǎn)品:

    • 生物活性

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research[2][3][4].

    IC50 & Target[1]

    hPPARγ

    0.93 μM (EC50)

    mouse PPARγ

    0.99 μM (EC50)

    hPPARδ

    43 μM (EC50)

    hPPARα

    100 μM (EC50)

    mouse PPARα

    100 μM (EC50)

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO EC50
    0.14 μM
    Compound: Pioglitazone
    Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay
    Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay
    		[PMID: 20656494]
    CHO EC50
    0.39 μM
    Compound: Pioglitazone
    Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
    Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay
    		[PMID: 21377875]
    COS-1 EC50
    0.39 μM
    Compound: 2
    Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay
    Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay
    		[PMID: 21130649]
    COS-7 EC50
    0.2 μM
    Compound: Pioglitazone
    Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
    Transactivation of human PPARgamma expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay
    		[PMID: 26595749]
    COS-7 EC50
    0.2 μM
    Compound: pioglitazone
    Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
    Transactivation of GAL4-fused human PPARgamma ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay
    		[PMID: 23130964]
    COS-7 EC50
    0.3 μM
    Compound: Pioglitazone
    Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay
    Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay
    		[PMID: 21873070]
    COS-7 EC50
    0.3 μM
    Compound: pioglitazone
    Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
    Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
    		[PMID: 20307981]
    COS-7 EC50
    0.32 μM
    Compound: Pioglitazone
    Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay
    Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay
    		[PMID: 27569195]
    COS-7 EC50
    0.5 μM
    Compound: Pioglitazone
    Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay
    Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay
    		[PMID: 27560282]
    CV-1 EC50
    580 nM
    Compound: Pioglitazone
    Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
    Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.
    		[PMID: 11720854]
    HEK293 EC50
    0.21 μM
    Compound: Pioglitazone
    Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay
    Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay
    		[PMID: 25333853]
    HEK293 EC50
    0.8 μM
    Compound: 4
    Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
    Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay
    		[PMID: 23102891]
    HEK293 EC50
    1.1 μM
    Compound: 1
    Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at Gal4 fused full length human PPARgamma LBD expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
    		[PMID: 28465099]
    HEK293 IC50
    22 μM
    Compound: 1
    Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay
    Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay
    		[PMID: 28465099]
    HepG2 EC50
    0.57 μM
    Compound: Pioglitazone
    Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
    Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay
    		[PMID: 22341573]
    HT-1080 IC50
    > 100 μM
    Compound: Pioglitazone
    Cytotoxic activity in human HT1080 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    Cytotoxic activity in human HT1080 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    		[PMID: 28395220]
    MDA-MB-231 IC50
    > 100 μM
    Compound: Pioglitazone
    Cytotoxic activity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    Cytotoxic activity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    		[PMID: 28395220]
    Mesenchymal stem cells EC50
    0.5 μM
    Compound: Pio
    Induction of adiponectin secretion in human BMMSC cells in presence of IDX induction medium by ELISA assay
    Induction of adiponectin secretion in human BMMSC cells in presence of IDX induction medium by ELISA assay
    		[PMID: 37077388]
    Mesenchymal stem cells EC50
    0.79 μM
    Compound: PIO
    Induction of adipogenesis in differentiated human BMMSC cells assessed as fold increase in adiponectin level in presence of IDX by ELISA
    Induction of adipogenesis in differentiated human BMMSC cells assessed as fold increase in adiponectin level in presence of IDX by ELISA
    		[PMID: 36475432]
    Mesenchymal stem cells EC50
    0.9 μM
    Compound: Pio
    Induction of adipogenesis in human differentiated BMMSC cells assessed as increase in adiponectin secretion and measured on 5 day in presence of IDX induction medium by ELISA
    Induction of adipogenesis in human differentiated BMMSC cells assessed as increase in adiponectin secretion and measured on 5 day in presence of IDX induction medium by ELISA
    		[PMID: 35859875]
    PC-3 IC50
    > 100 μM
    Compound: Pioglitazone
    Cytotoxic activity in human PC3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    Cytotoxic activity in human PC3 cells assessed as reduction in cell viability incubated for 3 days by MTT assay
    		[PMID: 28395220]
    THP-1 IC50
    > 50 μM
    Compound: Pioglitazone
    Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced IL-1beta secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA
    Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced IL-1beta secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA
    		[PMID: 23811092]
    THP-1 IC50
    18.6 μM
    Compound: Pioglitazone
    Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA
    Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion incubated for 2 hrs prior to PMA challenge measured after 72 hrs by ELISA
    		[PMID: 24531227]
    THP-1 IC50
    18.84 μM
    Compound: Pioglitazone
    Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA
    Antiinflammatory activity in human THP1 cells assessed as inhibition of PMA-induced MCP-1 secretion preincubated for 1 hr prior PMA-challenge measured after 48 hrs by ELISA
    		[PMID: 23811092]
    THP-1 IC50
    2.97 mM
    Compound: Pioglitazone
    Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation
    Inhibition of PMA-induced human THP1 monocytes differentiation in to macrophages assessed as macrophage metabolic activity preincubated for 6 hrs before PMA stimulation
    		[PMID: 30818268]
    體外研究
    (In Vitro)

    Pioglitazone (0.5 或 1 μM，5 天) 可完全阻止 AGEs (晚期糖基化終產(chǎn)物) 誘導(dǎo)的 β 細(xì)胞壞死和 caspase-3 的增加，從而避免 AGEs 導(dǎo)致的胰腺 β 細(xì)胞系 HIT-T15 的活力受損[2]。
    Pioglitazone (1 μM，1 h) 可刺激低葡萄糖濃度誘導(dǎo)的胰島素分泌，并降低 AGEs 培養(yǎng)細(xì)胞中的 GSSG/GSH 比值[2]。

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

    Pioglitazone (口服，10 或 30 mg/kg，每天一次，14 天) 可改善胰島素抵抗和糖尿病，這可能在肝臟中依賴脂質(zhì)運(yùn)載蛋白，但在骨骼肌中不依賴[3]。
    Pioglitazone (口服灌胃，10 mg/kg，每日一次，4 周) 可顯著減輕體重 (BW)、心肌肥厚、血糖水平升高并改善相關(guān)的血脂異常[4]。

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

    Animal Model: ob/ob and adipo-/- ob/ob mice with a C57Bl/6 background[3]
    Dosage: 10 or 30 mg/kg
    Administration: Oral gavage; once daily; 14 days
    Result: Showed no changes of serum-free fatty acid and triglyceride levels as well as adipocyte sizes in ob/ob and adipo-/- ob/ob C57BL/6 mice at 10 mg/kg but significantly reduced to a similar degree at 30 mg/kg.
    Also showed no changes of expressions of TNFα and resistin in adipose tissues of ob/ob and adipo-/- ob/ob mice at 10 mg/kg but decreased at 30 mg/kg.
    Animal Model: Male Wistar albino rats[4]
    Dosage: 10 mg/kg
    Administration: Oral gavage; once daily; 4 weeks
    Result: Decreased the elevated serum levels of both creatinine and creatine kinase-MB (CK-MB), TGF-β1 gene expression and regulated the expression of MMP-2/TIMP-2 system.
    Clinical Trial
    分子量

    356.44

    Formula

    C19H20N2O3S
    CAS 號(hào)
    性狀

    固體

    顏色

    White to off-white

    中文名稱

    吡格列酮；酮基匹格列酮
    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)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 : 25 mg/mL (70.14 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 2.8055 mL 14.0276 mL 28.0552 mL
    5 mM 0.5611 mL 2.8055 mL 5.6110 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。

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

      Solubility: 2.08 mg/mL (5.84 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (5.84 mM); 澄清溶液

      此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。

      以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

    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(qǐng)依序添加每種溶劑： 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (28.06 mM); Suspened solution; 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 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(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: 99.89%

    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
    DMSO 1 mM 2.8055 mL 14.0276 mL 28.0552 mL 70.1380 mL
    5 mM 0.5611 mL 2.8055 mL 5.6110 mL 14.0276 mL
    10 mM 0.2806 mL 1.4028 mL 2.8055 mL 7.0138 mL
    15 mM 0.1870 mL 0.9352 mL 1.8703 mL 4.6759 mL
    20 mM 0.1403 mL 0.7014 mL 1.4028 mL 3.5069 mL
    25 mM 0.1122 mL 0.5611 mL 1.1222 mL 2.8055 mL
    30 mM 0.0935 mL 0.4676 mL 0.9352 mL 2.3379 mL
    40 mM 0.0701 mL 0.3507 mL 0.7014 mL 1.7535 mL
    50 mM 0.0561 mL 0.2806 mL 0.5611 mL 1.4028 mL
    60 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1690 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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