1. JAK/STAT Signaling Stem Cell/Wnt
  2. STAT
  3. AS1517499

AS1517499 是有效的、可透过血脑屏障的 STAT6 磷酸化抑制剂,IC50 为 21 nM。

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AS1517499 Chemical Structure

AS1517499 Chemical Structure

CAS No. : 919486-40-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1045
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1 mg ¥380
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5 mg ¥910
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10 mg ¥1400
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25 mg ¥2100
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50 mg ¥3150
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100 mg ¥4725
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Top Publications Citing Use of Products

    AS1517499 purchased from MCE. Usage Cited in: J Exp Med. 2018 Aug 6;215(8):2175-2195.  [Abstract]

    Representative images of PCNA (green) and SMA (red) immunostaining of PASMCs cultured with DK-PGD2-treated Th2 cell medium with or without STAT6 inhibitor AS1517499.

    AS1517499 purchased from MCE. Usage Cited in: Respir Res. 2017 Sep 20;18(1):174.  [Abstract]

    BECs are pretreated with specific STAT6 inhibitor (AS1517499) or a selective IκB kinase inhibitor (IKK 16) for half an hour, then treated for 24 h in the presence or absence of 20 ng/mL IL-4. Immunofluorescence staining of MUC5AC protein is performed according to the Methods.

    查看 STAT 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AS1517499 is a potent and brain-permeable STAT6 phosphorylation inhibitor with an IC50 of 21 nM.

    IC50 & Target[1]

    STAT6

    21 nM (IC50)

    体外研究
    (In Vitro)

    AS1517499 显示出有效的 STAT6 抑制作用,IC50 值为 21 nM,还抑制 IL-4 诱导的小鼠脾脏 T 细胞 Th2 分化,IC50 值为 2.3 nM 且不影响 IL-12 诱导的 T 辅助细胞 1 (Th1) 分化。AS1517499 选择性抑制 Th2 分化而不影响 Th1 分化[1]
    在培养的人 BSM 细胞中,IL-13 (100 ng/mL) 引起 STAT6 的磷酸化和 RhoA 的上调,RhoA 是一种单体 GTP 酶,负责平滑肌收缩的 Ca2+ 敏感性:两者与 AS1517499 (100 nM)[2]共孵育可抑制事件。

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

    体内研究
    (In Vivo)

    在用卵清蛋白抗原主动致敏和反复攻击的 BALB/c 小鼠中,在最后一次抗原攻击后观察到支气管肺泡灌洗液中 IL-13 水平升高和支气管组织中 STAT6 磷酸化。这些小鼠具有增强的 BSM 对乙酰胆碱的收缩力以及支气管组织中 RhoA 的上调。在每次卵清蛋白暴露前 1 小时腹膜内注射 AS1517499 (10 mg/kg) 几乎完全抑制抗原诱导的 RhoA 和 BSM 高反应性上调[2]

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

    分子量

    397.86

    Formula

    C20H20ClN5O2

    CAS 号
    性状

    固体

    颜色

    White to light brown

    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
    In Vitro: 

    DMSO 中的溶解度 : ≥ 35 mg/mL (87.97 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5134 mL 12.5672 mL 25.1345 mL
    5 mM 0.5027 mL 2.5134 mL 5.0269 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

    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 (6.28 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。

      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% Corn Oil

      Solubility: ≥ 2.5 mg/mL (6.28 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,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 25.0 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,请直接配置工作液。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 (31.42 mM); 悬浊液; 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

    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: 99.17%

    参考文献
    Cell Assay
    [2]

    Normal human BSM cells (hBSMCs) are maintained in SmBM medium supplemented with 5% fetal bovine serum, 0.5 ng/mL human epidermal growth factor (hEGF), 5 μg/mL insulin, 2 ng/mL human fibroblast growth factor-basic (hFGF-b), 50 μg/mL gentamicin, and 50 ng/mL amphotericin B. Cells are maintained at 37°C in a humidified atmosphere (5% CO2), fed every 48 to 72 hours, and passaged when cells reached 90 to 95% confluence. Then the hBSMCs (passages 7-9) are seeded in 6-well plates and 8-well chamber slides at a density of 3,500 cells/cm2 and, when 80 to 85% confluence observed, cells are cultured without serum for 24 hours before addition of recombin is ant human IL-13. AS1517499 (100 nM) or its vehicle (0.3% DMSO) is treated 30 minutes before the addition of IL-13 (100 ng/mL). In some experiments, AS1517499 is treated 0 (co-incubation), 3, or 12 hours after the addition of IL-13. In another series of experiments, a selective Rho-kinase inhibitor Y-27632 (1 μM) or its vehicle (0.3% DMSO) is also applied 15 minutes before the IL-13 application. At the indicated time after the IL-13 treatment, cells are washed with PBS, immediately collected, and disrupted with 1× SDS sample buffer (250 μL/well), and used for Western blot analyses[2].

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

    Animal Administration
    [2]

    Mice[2]
    Male BALB/c mice are used. Preparation of a murine model of allergic bronchial asthma, which has an in vivo AHR, is performed. In brief, BALB/c mice (8 wk of age) are actively sensitized by intraperitoneal injections of 8 μg ovalbumin (OVA) with 2 mg Imject Alum on Day 0 and Day 5. The sensitized mice are challenged with aerosolized OVA-saline solution (5 mg/mL) for 30 minutes on Days 12, 16, and 20. A control group of mice received the same immunization procedure but inhaled saline aerosol instead of OVA challenge. The aerosol is generated with an ultrasonic nebulizer and introduced to a Plexiglas chamber box (130×200 mm, 100 mm height) in which the mice are placed. Animals also received intraperitoneal injection with AS1517499 (1 or 10 mg/kg/d; dissolved in 20% DMSO in saline) or its vehicle 1 hour before each antigen inhalation (Days 12, 16, and 20). Twenty-four hours after the last OVA challenge, mice are killed by exsanguination from abdominal aorta under urethane (1.6 g/kg, intraperitoneally) anesthesia.

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

    参考文献

    AS1517499 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 2.5134 mL 12.5672 mL 25.1345 mL 62.8362 mL
    5 mM 0.5027 mL 2.5134 mL 5.0269 mL 12.5672 mL
    10 mM 0.2513 mL 1.2567 mL 2.5134 mL 6.2836 mL
    15 mM 0.1676 mL 0.8378 mL 1.6756 mL 4.1891 mL
    20 mM 0.1257 mL 0.6284 mL 1.2567 mL 3.1418 mL
    25 mM 0.1005 mL 0.5027 mL 1.0054 mL 2.5134 mL
    30 mM 0.0838 mL 0.4189 mL 0.8378 mL 2.0945 mL
    40 mM 0.0628 mL 0.3142 mL 0.6284 mL 1.5709 mL
    50 mM 0.0503 mL 0.2513 mL 0.5027 mL 1.2567 mL
    60 mM 0.0419 mL 0.2095 mL 0.4189 mL 1.0473 mL
    80 mM 0.0314 mL 0.1571 mL 0.3142 mL 0.7855 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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    产品名称:
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    目录号:
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