2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Neuronal Signaling Membrane Transporter/Ion Channel Autophagy Apoptosis
  3. PPAR TRP Channel Autophagy Ferroptosis
  4. Rosiglitazone maleate

Rosiglitazone maleate  (Synonyms: 马来酸罗格列酮; BRL 49653C)

目录号: HY-14600 纯度: 99.88%
COA 产品使用指南

摩尔计算器

Rosiglitazone maleate (BRL 49653C) 是一种有效的，选择性的 PPARγ 激活剂，对 PPARγ1，PPARγ2 和 PPARγ 的 EC50 值分别为 30 nM，100 nM 和 60 nM，对 PPARγ 的 Kd 值约为 40 nM；Rosiglitazone maleate 同时为 TRP channels 的调节剂，可抑制 TRPM2, TRPM3 的活性，激活 TRPC5。

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Rosiglitazone maleate Chemical Structure

Rosiglitazone maleate Chemical Structure

CAS No. : 155141-29-0

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50 mg ￥600
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200 mg ￥1800
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Customer Review

Other Forms of Rosiglitazone maleate:

Rosiglitazone maleate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 84 篇科研文献

WB
IF
Cell Viability Assay

    Rosiglitazone maleate purchased from MCE. Usage Cited in: Carcinogenesis. 2023 Mar 31;bgad015.  [Abstract]

    Rosiglitazone (ROSI; 15, 30, 60, 120, 240 µM; 24 h) significantly inhibits the growth of NCI-H929 and OPM-2 cells.

    Rosiglitazone maleate purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    Protein levels of sAPPα and sAPPβ are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).

    Rosiglitazone maleate purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    Protein levels of BACE1 and APP are measured by western blot assay in cerebral cortex of 12-month-old AD mice with different treatments (RSG and GW9662).

    Rosiglitazone maleate purchased from MCE. Usage Cited in: Eur J Pharmacol. 2019 Jan 15;843:134-144.  [Abstract]

    PPARγ level is determined by IF assay in 3×Tg-AD mice, 3×Tg-AD mice with RSG treatment, 3×Tg-AD-KO mice, 3×Tg-AD-KO mice with GW9662 stimulation.

    Rosiglitazone maleate purchased from MCE. Usage Cited in: Free Radic Biol Med. 2018 Aug 21;126:259-268.  [Abstract]

    Laser confocal microscope is performed to measure MMP indicated with the ratio of JC-1 Red/JC-1 Green. Nuclei are counterstained with DAPI (blue). Bar graphs represent the mean ± SD of red/green fluorescence intensity.

    Rosiglitazone maleate purchased from MCE. Usage Cited in: Front Mol Neurosci. 2017 Sep 14;10:293.  [Abstract]

    Rosiglitazone enhances the phosphorylation of insulin receptor substrate 1 (IRS1, phosphorylated at Ser 636/639), which is considered to be the main activator of the Akt/mTOR pathway by IGF-1R.

    查看 PPAR 亚型特异性产品:

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    PPARα PPARβ/δ PPARγ PPAR PPARδ

    查看 TRP Channel 亚型特异性产品:

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    TRPC TRPM TRPV TRPA TRPML

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Rosiglitazone maleate (BRL 49653C) is a potent and selective activator of PPARγ, with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, and a Kd of appr 40 nM for PPARγ; Rosiglitazone maleate is also an modulator of TRP channels, inhibits TRP melastatin 2 (TRPM2), TRPM3 and activates TRP canonical 5 (TRPC5).

    IC50 & Target[1]

    PPARγ1

    30 nM (EC50)

    PPARγ2

    100 nM (EC50)

    体外研究
    (In Vitro)

    Rosiglitazone maleate 是一种有效的选择性 PPARγ 激活剂，对 PPARγ1 和 PPARγ2 的 EC50 分别为 30 nM 和 100 nM，Kd 约为 40 nM对于 PPARγ。Rosiglitazone (BRL49653，0.1，1，10 μM) 促进 C3H10T1/2 干细胞分化为脂肪细胞[1]。
    Rosiglitazone (Compound 6) 激活 PPARγ，EC50 为 60 nM[2]。
    Rosiglitazone (1 μM) 激活 PPARγ，后者结合 NF-α1 启动子以激活神经元中的基因转录。Rosiglitazone (1 μM) 还保护 Neuro2A 细胞和海马神经元免受氧化应激，并以 NF-α1 依赖性方式上调 BCL-2 表达[3]。
    Rosiglitazone 完全抑制 TRPM3，针对硝苯地平和 PregS 诱发的活性，IC50 值为 9.5 和 4.6 μM，但这种作用不是通过 PPARγ 产生的。Rosiglitazone 在较高浓度下抑制 TRPM2，IC50 约为 22.5 μM。Rosiglitazone 是 TRPC5 通道的强刺激剂，EC50 为 ～30 μM[4]。

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

    Rosiglitazone maleate 相关抗体:
    体内研究
    (In Vivo)

    Rosiglitazone (5 mg/kg，po) 降低糖尿病大鼠的血清葡萄糖。Rosiglitazone 还能降低糖尿病组的 IL-6、TNF-α 和 VCAM-1 水平。与糖尿病和 Los 处理组相比，Rosiglitazone 与氯沙坦联合使用可增加血糖。Rosiglitazone 显著改善内皮功能障碍，表现在对 PE 和 Ang II 的收缩反应显著降低以及 ACh 诱发的松弛增强在从糖尿病大鼠分离的主动脉中[5]。

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

    473.50

    Formula

    C22H23N3O7S
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    马来酸罗格列酮
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (211.19 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.1119 mL 10.5597 mL 21.1193 mL
    5 mM 0.4224 mL 2.1119 mL 4.2239 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    • 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 (5.28 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。

      以 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 (5.28 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。

      以 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

    只
    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）。

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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
    参考文献
    Kinase Assay
    [1]

    cDNA encoding amino acids 174-475 of PPARγ1 is amplified via polymerase chain reaction and inserted into bacterial expression vector pGEX-2T. GST-PPARγ LBD is expressed in BL21(DE3)plysS cells and extracts. For saturation binding analysis, bacterial extracts (100 μg of protein) are incubated at 4°C for 3 h in buffer containing 10 mM Tris (pH 8.0), 50 mM KCl, 10 mM dithiothreitol with [3H]-BRL49653 (specific activity, 40 Ci/mmol) in the presence or absence of unlabeled Rosiglitazone. Bound is separated from free radioactivity by elution through 1-mL Sephadex G-25 desalting columns. Bound radioactivity eluted in the column void volume and is quantitated by liquid scintillation counting[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [1]

    C3H10T1/2 cells are grown in a 24-well plate in DME medium supplemented with 10% fetal calf serum. Medium and compound (Rosiglitazone) are exchanged every 3 days. Cells are stained at day 7 with Oil Red O and photographed[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Rats are intravenously injected with 38 mg/kg streptozotocin and after 48 h, diabetes is identified by urinary glucosuria and then random blood sugar is measured and this day is regarded as day 0. Animals with a serum glucose level of 220-300 mg/dL are selected to be used in this study. Rats are randomly separated into five groups for daily drug administration for 8 weeks: group 1: control nondiabetic rats given a vehicle only (0.5 mL/kg of 0.5% carboxy methyl celleluse orally), group 2: control diabetic rats given a vehicle, group 3: diabetic rats receiving Rosiglitazone (5 mg/kg orally), group 4: diabetic rats receiving losartan (2 mg/kg, orally), and group 5: diabetic rats receiving both Rosiglitazone and losartan[2].

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

    Rosiglitazone maleate 相关分类

    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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.1119 mL 10.5597 mL 21.1193 mL 52.7983 mL
    5 mM 0.4224 mL 2.1119 mL 4.2239 mL 10.5597 mL
    10 mM 0.2112 mL 1.0560 mL 2.1119 mL 5.2798 mL
    15 mM 0.1408 mL 0.7040 mL 1.4080 mL 3.5199 mL
    20 mM 0.1056 mL 0.5280 mL 1.0560 mL 2.6399 mL
    25 mM 0.0845 mL 0.4224 mL 0.8448 mL 2.1119 mL
    30 mM 0.0704 mL 0.3520 mL 0.7040 mL 1.7599 mL
    40 mM 0.0528 mL 0.2640 mL 0.5280 mL 1.3200 mL
    50 mM 0.0422 mL 0.2112 mL 0.4224 mL 1.0560 mL
    60 mM 0.0352 mL 0.1760 mL 0.3520 mL 0.8800 mL
    80 mM 0.0264 mL 0.1320 mL 0.2640 mL 0.6600 mL
    100 mM 0.0211 mL 0.1056 mL 0.2112 mL 0.5280 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.

    Keywords:

    Rosiglitazone155141-29-0BRL 49653C马来酸罗格列酮PPARTRP ChannelAutophagyFerroptosisPeroxisome proliferator-activated receptorsTransient receptor potential channelsInhibitorinhibitorinhibit

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