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  3. Pioglitazone

Pioglitazone  (Synonyms: 吡格列酮; U 72107)

目录号: HY-13956 纯度: 99.89%
COA 产品使用指南

Pioglitazone (U 72107) 是一种具有口服活性的选择性 PPARγ (peroxisome proliferator-activated receptor) 激动剂,高亲和力结合到 PPARγ 配体结合域,作用于人和鼠 PPARγEC50 分别为 0.93 和 0.99 μM。Pioglitazone 可用于糖尿病研究。

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Pioglitazone Chemical Structure

Pioglitazone Chemical Structure

CAS No. : 111025-46-8

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Customer Review

MCE 顾客使用本产品发表的 29 篇科研文献

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 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    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)

    细胞效力
    (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]
    体外研究
    (In Vitro)

    Pioglitazone (0.5 或 1 μM,5 天) 可完全阻止 AGEs (晚期糖基化终产物) 诱导的 β 细胞坏死和 caspase-3 的增加,从而避免 AGEs 导致的胰腺 β 细胞系 HIT-T15 的活力受损[2]
    Pioglitazone (1 μM,1 h) 可刺激低葡萄糖浓度诱导的胰岛素分泌,并降低 AGEs 培养细胞中的 GSSG/GSH 比值[2]

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

    体内研究
    (In Vivo)

    Pioglitazone (口服,10 或 30 mg/kg,每天一次,14 天) 可改善胰岛素抵抗和糖尿病,这可能在肝脏中依赖脂质运载蛋白,但在骨骼肌中不依赖[3]
    Pioglitazone (口服灌胃,10 mg/kg,每日一次,4 周) 可显著减轻体重 (BW)、心肌肥厚、血糖水平升高并改善相关的血脂异常[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 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    吡格列酮;酮基匹格列酮

    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
    细胞实验: 

    DMSO 中的溶解度 : 25 mg/mL (70.14 mM; 超声助溶 (<60°C); 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 2.8055 mL 14.0276 mL 28.0552 mL
    5 mM 0.5611 mL 2.8055 mL 5.6110 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

    动物实验:

    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: 2.08 mg/mL (5.84 mM); 悬浊液; 超声助溶

      此方案可获得 2.08 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 20.8 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% Corn Oil

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

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (28.06 mM); Suspened solution; 超声助溶

    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: 99.89%

    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 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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