1. GPCR/G Protein Immunology/Inflammation
  2. CXCR
  3. SB225002

SB225002 是一种有效的选择性 CXCR2 非肽拮抗剂,抑制 125I-IL-8 和 CXCR2 结合的 IC50 为 22 nM。

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SB225002 Chemical Structure

SB225002 Chemical Structure

CAS No. : 182498-32-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥605
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5 mg ¥546
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10 mg ¥770
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50 mg ¥2900
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100 mg ¥4538
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200 mg ¥6575
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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 29 篇科研文献

IF

    SB225002 purchased from MCE. Usage Cited in: J Autoimmun. 2018 May;89:30-40.  [Abstract]

    The blockade of neutrophil infiltration and intracutaneous injection of exogenous galectin-3 ameliorates skin inflammation in galectin 3-/- mice
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SB225002, a potent, selective and non-peptide CXCR2 antagonist, inhibits 125I-IL-8 binding to CXCR2 with an IC50 of 22 nM.

    IC50 & Target[1]

    125I-IL-8-CXCR2

    22 nM (IC50, in CHO cell membrane)

    体外研究
    (In Vitro)

    SB225002 (SB 225002) 是 125I-IL-8 与 CXCR2 结合的拮抗剂,IC50=22 nM。SB225002 显示出比 CXCR1 和其他四个测试的 7-TMR 高 150 倍以上的选择性。SB225002 是兔 CXCR2 的有效拮抗剂,抑制兔 PMN 趋化性以响应最佳浓度的人 IL-8 或 GROα (IC50 值分别为 30 和 70 nM。在这些细胞 (PMN,HL60,CXCR1-RBL-2H3),SB225002 对 IL-8 和 GROα 介导的钙动员产生浓度依赖性抑制,IC50 值分别为 8 和 10 nM。在 3ASubE 细胞中用 CXCR2 稳定转染后,SB 225002 剂量依赖性地抑制由 GROα 和 IL-8 诱导的钙动员,IC50 值分别为 20 和 40 nM[1]
    用 SB225002 处理的 WHCO1 细胞显示细胞增殖减少 40%。用 400 nM SB225002 (SB 225002) 阻断 WHCO1 细胞中的 CXCR2 信号,可显著降低细胞增殖约 40% 至 50%[2]

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

    体内研究
    (In Vivo)

    SB225002 (SB 225002) 选择性阻断兔体内 IL-8 诱导的嗜中性粒细胞边缘化[1]
    使用选择性拮抗剂 SB225002 (2 mg/kg) 或中和 CXCR2 抗血清可阻断 CXCR2。CXCR2 拮抗剂 SB225002 减少了西方饮食的 ApoE / 小鼠和正常饮食的野生型小鼠[3]的缺血半球中的中性粒细胞计数。SB225002 显著减轻小胶质细胞活化和 BBB 损伤,增加髓鞘形成,并减少 LPS 致敏 HI 后白质中的星形胶质细胞增生[4]

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

    分子量

    352.14

    Formula

    C13H10BrN3O4

    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, stored under nitrogen

    *In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (283.98 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 2.8398 mL 14.1989 mL 28.3978 mL
    5 mM 0.5680 mL 2.8398 mL 5.6796 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 (stored under nitrogen)。-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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (7.10 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。

    • 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 (5.91 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。

      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。
    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)。

    *In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

    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: 99.87%

    参考文献
    Kinase Assay
    [1]

    CHO-CXCR1 and CHO-CXCR2 membranes are prepared. Assays are performed in 96-well microtiter plates where the reaction mixture contained 1.0 μg/mL membrane protein in 20 mM Bis-Tris-propane, pH 8.0, with 1.2 mM MgSO4, 0.1 mM EDTA, 25 mM NaCl, and 0.03% CHAPS and SB 225002 (10 mM stock in Me2SO) added at the indicated concentrations, the final Me2SO concentration is <1% under standard binding conditions. Binding is initiated by addition of 0.25 nM 125I-IL-8 (2,200 Ci/mmol). After 1-h incubation at room temperature the plate is harvested using a Tomtec 96-well harvester onto a glass fiber filtermat blocked with 1% polyethyleneimine, 0.5% BSA and washed three times with 25 mM NaCl, 10 mM Tris•HCl, 1 mM MgSO4, 0.5 mMEDTA, 0.03% CHAPS, pH 7.4. The filter is dried, sealed in a sample bag containing 10 mL of Wallac 205 Betaplate liquid scintillation fluid, and counted with a Wallac 1205 Betaplate liquid scintillation counter[1].

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

    Cell Assay
    [2]

    Three esophageal squamous cell carcinoma cell lines WHCO1, WHCO5, and WHCO6 originally established from surgical biopsies of primary esophageal squamous cell carcinomas are cultured in DMEM containing 10% FCS at 37°C in a humidified atmosphere of 5% CO2. MTT assays are carried out using the Cell Proliferation kit. Briefly, 1.5×103 cells are plated in 96-well plates in a final volume of 180 μL DMEM per well. SB 225002 (400 nM) is added to cells and 0.001% DMSO (solvent) is added as a control. After the indicated incubation period, 18 μL of the MTT labeling reagent (final concentration 0.5 mg/mL) is added to each well and incubated for 4 hours in a humidified atmosphere. One hundred eighty microliters of the solubilization solution are added to each well and the plates are left overnight at 37°C. The spectrophotometric absorbance of samples is measured at 595 nm using a microtiter plate reader[2].

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

    Animal Administration
    [3][4]

    Mice[3]
    Male 7-8 weeks old wildtype (C57BL/6J, Harlan) and ApoE−/− mice, which are generated on the same C57BL/6 background, are either fed with a normal chow or a cholesterol rich chow for 6 weeks and submitted to 20 min of left-sided middle cerebral artery occlusion (MCAO) or sham surgery. Animals are randomly attributed to treatment paradigms, and experimenters are blinded at all stages of interventions and data analysis. The selective CXCR2 antagonist SB225002 (2 mg/kg) or vehicle (1% DMSO in PBS) is injected intraperitoneally (i.p.) at 0, 24 and 48 hours post-ischemia. In other experiments, CXCR2 is specifically blocked by i.p. injection of a neutralizing rabbit anti-CXCR2 serum (300 μL) at 0 hours, 24 hours and 48 hours post-ischemia. In the latter studies, normal rabbit serum (NRS) served as control. In some experiments, neutrophils are depleted by i.p. injection of 200 μg anti-mouse Ly6G 24 hours before and 24 hours after ischemia. In these experiments, 200 μg of an isotype control antibody is delivered as control.
    Rats[4]
    In this study, 10-12 Sprague-Dawley rat pups per dam are used. The pups receive intraperitoneal injections of SB225002 (1 or 3 mg/kg, diluted in NS containing 0.33 % Tween 80) or vehicle (NS solution containing 0.33 % Tween 80) 30 min before lipopolysaccharide (LPS) administration and immediately after hypoxic ischemia (HI). The pups are randomly assigned to four groups: control (pups unexposed to LPS or HI, N=14), vehicle (NS injections 30 min before LPS administration and immediately after HI, N=18), and SB-1 (1 mg/kg, N=14) and SB-3 (3 mg/kg, N=18) (SB225002 injections 30 min before LPS administration and immediately after HI).

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

    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 (stored under nitrogen)。-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 2.8398 mL 14.1989 mL 28.3978 mL 70.9945 mL
    5 mM 0.5680 mL 2.8398 mL 5.6796 mL 14.1989 mL
    10 mM 0.2840 mL 1.4199 mL 2.8398 mL 7.0994 mL
    15 mM 0.1893 mL 0.9466 mL 1.8932 mL 4.7330 mL
    20 mM 0.1420 mL 0.7099 mL 1.4199 mL 3.5497 mL
    25 mM 0.1136 mL 0.5680 mL 1.1359 mL 2.8398 mL
    30 mM 0.0947 mL 0.4733 mL 0.9466 mL 2.3665 mL
    40 mM 0.0710 mL 0.3550 mL 0.7099 mL 1.7749 mL
    50 mM 0.0568 mL 0.2840 mL 0.5680 mL 1.4199 mL
    60 mM 0.0473 mL 0.2366 mL 0.4733 mL 1.1832 mL
    80 mM 0.0355 mL 0.1775 mL 0.3550 mL 0.8874 mL
    100 mM 0.0284 mL 0.1420 mL 0.2840 mL 0.7099 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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    目录号:
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