2. GPCR/G Protein
  3. Adenosine Receptor
  4. ZM241385

ZM241385 是一种有效的，高亲和力的选择性的腺苷 A2AR 拮抗剂，其 Ki 值为 1.4 nM。

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ZM241385 Chemical Structure

ZM241385 Chemical Structure

CAS No. : 139180-30-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥600
In-stock
10 mg ￥860
In-stock
50 mg ￥3188
In-stock
100 mg ￥4725
In-stock
200 mg 现货 询价
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of ZM241385:

ZM241385 相关抗体

Top Publications Citing Use of Products

    ZM241385 purchased from MCE. Usage Cited in: Ecotoxicol Environ Saf. 2022 Dec 12;249:114410.  [Abstract]

    ZM241385 (10 μM) significantly decreases the levels of E-cad, increases the N-cad, Vimentin, and α-SMA levels by inhibiting A2aR, in A549 cells.

    查看 Adenosine Receptor 亚型特异性产品:

    查看所有亚型
    Adenosine A1 receptor (A1R) Adenosine A2A receptor (A2AR) Adenosine A2B receptor (A2BR) Adenosine A3 receptor (A3R)

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    ZM241385 is a potent, high affinity and selective adenosine A2a receptor (A2AR) antagonist with a Ki value of 1.4 nM[1][2][3].

    IC50 & Target[2] [1]

    A2AR

    1.4 nM (Ki)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    CHO EC50
    > 100000 nM
    Compound: 1, ZM 241385
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    Agonist activity at human dopamine D2L receptor expressed in CHO cell membranes incubated for 1 hr by [35S]GTPgammaS binding assay
    		[PMID: 25490054]
    CHO IC50
    0.678 nM
    Compound: 1; ZM 241385
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Antagonist activity against human adenosine A2A receptor expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    1.45 nM
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    CHO IC50
    33 nM
    Compound: 1, ZM 241385
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    Inhibition of human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of NECA-induced cAMP accumulation incubated for 30 mins by fluorescence assay
    		[PMID: 25490054]
    CHO IC50
    42 nM
    Compound: 5, ZM 241385
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    Antagonist activity at recombinant human adenosine A2A receptor expressed in CHO cells assessed as inhibition of NECA-induced cAMP production after 60 mins
    		[PMID: 23602401]
    CHO IC50
    48 nM
    Compound: 1; ZM 241385
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    Inverse agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of cAMP accumulation measured after 150 mins in presence of [3H]cAMP by scintillation counting method
    		[PMID: 27933962]
    体外研究
    (In Vitro)

    ZM241385 (1 μM; 24-48 hours; PC12 cells) treatment reverses the phenomenon that A2AR agonist CGS21680 significantly upregulates A2AR mRNA and protein levels[1].

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

    ZM241385 相关抗体:

    RT-PCR[1]

    Cell Line: PC12 cells
    Concentration: 1 μM
    Incubation Time: 24 hours
    Result: Suppressed the increased A2AR mRNA levels engendered by CGS21680.

    Western Blot Analysis[1]

    Cell Line: PC12 cells
    Concentration: 1 μM
    Incubation Time: 48 hours
    Result: Decreased A2AR protein levels
    体内研究
    (In Vivo)

    ZM241385 (0.2 μg/mouse, 0.4 μg/mouse; intraperitoneal injection; every day; for 11 weeks; female C57BL/6 WT mice) treatment decreases tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC[4].

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

    Animal Model: Female C57BL/6 WT mice received 4-nitroquinoline-N-oxide[4]
    Dosage: 0.2 μg/mouse, 0.4 μg/mouse
    Administration: Intraperitoneal injection; every day; for 11 weeks
    Result: Decreased tumor volume, activates CD8+ T cells and reduces the frequency of splenic MDSC.
    分子量

    337.34

    Formula

    C16H15N7O2
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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 : 125 mg/mL (370.55 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 2.9644 mL 14.8218 mL 29.6437 mL
    5 mM 0.5929 mL 2.9644 mL 5.9287 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 6.25 mg/mL (18.53 mM); 澄清溶液

    • 方案 二

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.17 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。

      以 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。

    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： 50% PEG300    50% Saline

      Solubility: 12.5 mg/mL (37.05 mM); 澄清溶液; 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

    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）。
    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: 99.26%

    COA (283 KB) LCMS (122 KB)

    产品使用指南 (1538 KB)
    参考文献

    ZM241385 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, 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 2.9644 mL 14.8218 mL 29.6437 mL 74.1092 mL
    5 mM 0.5929 mL 2.9644 mL 5.9287 mL 14.8218 mL
    10 mM 0.2964 mL 1.4822 mL 2.9644 mL 7.4109 mL
    15 mM 0.1976 mL 0.9881 mL 1.9762 mL 4.9406 mL
    20 mM 0.1482 mL 0.7411 mL 1.4822 mL 3.7055 mL
    25 mM 0.1186 mL 0.5929 mL 1.1857 mL 2.9644 mL
    30 mM 0.0988 mL 0.4941 mL 0.9881 mL 2.4703 mL
    40 mM 0.0741 mL 0.3705 mL 0.7411 mL 1.8527 mL
    50 mM 0.0593 mL 0.2964 mL 0.5929 mL 1.4822 mL
    60 mM 0.0494 mL 0.2470 mL 0.4941 mL 1.2352 mL
    80 mM 0.0371 mL 0.1853 mL 0.3705 mL 0.9264 mL
    100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7411 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:

    ZM241385139180-30-6ZM 241385ZM-241385Adenosine ReceptorP1 receptorInhibitorinhibitorinhibit

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    目录号：
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