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

Reparixin  (Synonyms: 瑞帕利辛; Repertaxin; DF 1681Y)

目录号: HY-15251 纯度: 99.95%
COA 产品使用指南

Reparixin是趋化因子受体 CXCR1CXCR2 激活的非竞争性变构抑制剂,IC50 分别为1 和 100 nM。

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Reparixin Chemical Structure

Reparixin Chemical Structure

CAS No. : 266359-83-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1231
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2 mg ¥790
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5 mg ¥1600
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10 mg ¥2750
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25 mg ¥4800
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50 mg ¥7440
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Customer Review

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Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 48 篇科研文献

Proliferation Assay
IF

    Reparixin purchased from MCE. Usage Cited in: Front Immunol. 17 October 2022.

    In HL-1 cells, when DSS and Reparixin (100nM) are applied in combination, the high expression levels of NF-κB, COX-2, ICAM-1 and VCAM-1 induced by OGD/R are further inhibited compared with that of DSS alone.

    Reparixin purchased from MCE. Usage Cited in: J Gastroenterol Hepatol. 2018 Feb;33(2):431-442.  [Abstract]

    The effects of TRAF2 overexpression with or without Reparixin (100 nM), or BAY 11-7082 (30 μM) on the migration and invasion of AGS cell are examined by transwell assay.

    Reparixin purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 21;8(36):60210-60222.  [Abstract]

    Migration assay of MDA-MB-231 cells treated 0.1 uM of Reparixin in CM from fibroblasts or macrophages with TCM of MDA-MB-231 cells using the Oris Cell migration kit.

    Reparixin purchased from MCE. Usage Cited in: Oncogenesis. 2016 Jun 13;5(6):e234.  [Abstract]

    The effects of Reparixin (100 nM) on the migration of OLFM4-depleted gastric cancer cells are detected by transwell assay.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.

    IC50 & Target[1][5]

    CXCR1wt

    5.6 nM (IC50, in L1.2 cells)

    CXCR1Ile43Val

    80 nM (IC50, in L1.2 cells)

    CXCR1

    1 nM (IC50, in cells)

    CXCR2

    ∼100 nM (IC50, in cells)

    体外研究
    (In Vitro)

    Reparixin 是一种有效的功能性抑制剂,可抑制 CXCL8 诱导的人类 PMN 生物活性,对 CXCR1 具有显著的选择性 (约 400 倍),如 CXCR1/L1.2 和 CXCR2/L1.2 转染细胞和人类的特定实验所示PMN。Reparixin 在表达 Ile43Val CXCR1 突变体的 L1.2 细胞中的功效显著降低 (对 CXCR1 wt 和 CXCR1 Ile43Val 的 IC50 值分别为 5.6 nM 和 80 nM)[1]。Reparixin 是一种非竞争性 IL-8 受体变构抑制剂,其抑制 CXCR1 活性的功效比 CXCR2[2]高 400 倍。

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

    体内研究
    (In Vivo)

    Reparixin 是 CXCL8 受体 CXCR1CXCR2 激活的抑制剂,已被证明可以减轻各种损伤模型中的炎症反应。自发性高血压大鼠 (SHR) 每天皮下注射 Reparixin (5 mg/kg),持续 3 周。Reparixin 有效降低收缩压并增加血流量[3]。Reparixin 降低小鼠大脑中动脉闭塞/再灌注 (MCAo) 后大脑中 IL-1β 的水平。条形表示在接受或未接受 MCAo 并用载体或 Reparixin (30 mg/kg,sc) 预处理的小鼠脑组织中通过 ELISA 测量的 IL-1β 水平 (pg/100 mg)[4]

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

    Clinical Trial
    分子量

    283.39

    Formula

    C14H21NO3S

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    瑞帕利辛

    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 : ≥ 100 mg/mL (352.87 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)

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

    * "≥" 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 3.5287 mL 17.6435 mL 35.2871 mL
    5 mM 0.7057 mL 3.5287 mL 7.0574 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 (8.82 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (8.82 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 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

    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: 99.95%

    参考文献
    Cell Assay
    [1]

    L1.2 Cell suspension (1.5-3×106 cells/mL) is incubated at 37°C for 15 min in the presence of vehicle or of Reparixin (1 nM-1μM) and next seeded in triplicates in the upper compartment of the chemotactic chamber. Different agonists are seeded in the lower compartment of the chamber at the following concentrations: 1 nM CXCL8, 0.03 nM fMLP, 10 nM CXCL1, 2.5 nM CCL2, 30 nM C5a. The chemotactic chamber is incubated at 37°C in air with 5% CO2 for 45 min (human PMNs) or 2 h (monocytes). At the end of incubation, the filter is removed, fixed, and stained and five oil immersion fields at high magnification (100×) are counted for each migration well after sample coding. L1.2 migration is evaluated using 5 μm pore size Transwell filters[1].

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

    Animal Administration
    [3][4]

    Rats[3]
    The Reparixin-treated group contained 5 SHR (SHR-R), where equal numbers of normal saline-treated SHR (SHR-N) and WKY (WKY-N) served as controls. Eighteen-week-old SHR received a subcutaneous injection of Reparixin (5 mg/kg) once per day for 3 weeks. Reparixin effects on blood flow, blood pressure and body weight are measured before treatment and then weekly until 1 week after the final injection. The effect of Reparixin on the expression of hypertension-related mediators in thoracic aortas, as well as nitric oxide (NO) plasma levels, is examined 1 week after the final injection.
    Mice[4]
    C57BL/6J mice (8-10 weeks old/20-25 g) are used. The subcutaneous administration of Reparixin (30 mg/kg) is performed 60 minutes before cerebral ischemia induction. The animals are divided into the following three experimental groups: Sham (i.e., the group in which the arteries are visualized, but there is no occlusion of the middle cerebral artery), Vehicle (i.e., the group pre-treated with the vehicle, phosphate buffer solution, 60 minutes before MCAo) and Reparixin (i.e., the group pre-treated with the drug 60 minutes before MCAo). To evaluate neurological signs secondary to MCAo, the animals are assessed with the SHIRPA battery 24 h after reperfusion.

    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。-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 3.5287 mL 17.6435 mL 35.2871 mL 88.2176 mL
    5 mM 0.7057 mL 3.5287 mL 7.0574 mL 17.6435 mL
    10 mM 0.3529 mL 1.7644 mL 3.5287 mL 8.8218 mL
    15 mM 0.2352 mL 1.1762 mL 2.3525 mL 5.8812 mL
    20 mM 0.1764 mL 0.8822 mL 1.7644 mL 4.4109 mL
    25 mM 0.1411 mL 0.7057 mL 1.4115 mL 3.5287 mL
    30 mM 0.1176 mL 0.5881 mL 1.1762 mL 2.9406 mL
    40 mM 0.0882 mL 0.4411 mL 0.8822 mL 2.2054 mL
    50 mM 0.0706 mL 0.3529 mL 0.7057 mL 1.7644 mL
    60 mM 0.0588 mL 0.2941 mL 0.5881 mL 1.4703 mL
    80 mM 0.0441 mL 0.2205 mL 0.4411 mL 1.1027 mL
    100 mM 0.0353 mL 0.1764 mL 0.3529 mL 0.8822 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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