1. GPCR/G Protein Immunology/Inflammation
  2. CCR
  3. RS102895

RS102895 是一种有效的 CCR2 拮抗剂,IC50 值为 360 nM,对 CCR1 无作用。

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RS102895 Chemical Structure

RS102895 Chemical Structure

CAS No. : 300815-41-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥825
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5 mg ¥750
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10 mg ¥1200
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25 mg ¥2200
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Other Forms of RS102895:

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Top Publications Citing Use of Products

    RS102895 purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Sep;16(3):3387-3394.  [Abstract]

    Western blot analysis of the protein expression of ERK1/2, p ERK1/2, p38 and p p38 is performed using SDS PAGE.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.

    IC50 & Target[1]

    CCR2

    360 nM (IC50)

    CCR1

    17800 nM (IC50)

    Human α1a receptor

    130 nM (IC50)

    Human α1d receptor

    320 nM (IC50)

    5HT-1a receptor

    470 nM (IC50)

    体外研究
    (In Vitro)

    RS102895 is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1. RS102895 also inhibits human α1a and α1d receptors, rat brain cortex 5HT1a receptor in cells with IC50s of 130, 320, 470 nM, respectively. RS102895 suppresses wild type and D284N mutant MCP-1 receptor (IC50, 550 nM and 568 nM, respectively), less potently inhibits D284A MCP-1 receptor (IC50, 1892 nM), and has no effects on E291A, E291Q, D284A/E291A or D284N/E291Q (IC50, >100,000 nM)[1]. RS102895 ameliorates the increased extracellular matrix (ECM) protein expression by inhibition of CCR2 at 10 μM, and obviously blocks fibronectin and type IV collagen protein expression in high glucose (HG)-stimulated mesangial cells (MCs) at 1 or 10 μM. RS102895 (10 μM) also abrogates the increased TGF-1 levels in MCs treated with MCP-1[2].

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

    体内研究
    (In Vivo)

    RS102895 (3 g/L) causes progressive decrease in pain threshold in rats with bone cancer pain (BCP) at day 3-9 after surgery via intrathecal injection, but the pain threshold increases after 12 days. RS102895 also potently reverses the pattern of NR2B, nNOS, and SIGIRR expression in spinal cord[3].

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

    分子量

    390.40

    Formula

    C21H21F3N2O2

    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

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 250 mg/mL (640.37 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)

    Ethanol 中的溶解度 : 50 mg/mL (128.07 mM; 超声助溶 (<60°C))

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5615 mL 12.8074 mL 25.6148 mL
    5 mM 0.5123 mL 2.5615 mL 5.1230 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 (protect from light)。-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

    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
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.97%

    参考文献
    Cell Assay
    [2]

    Transfected mesangial cells (MCs) are serum restricted for 24 h, after which the medium is replaced by serum-free DMEM containing normal glucose (NG; 5.6 mM), NG+Mannitol (NG+M; 24.4 mM), or high glucose (HG; 30 mM). In addition, nontransfected MCs are cultured under NG, NG+M, or HG with or without RS102895 or anti-TGF-1 antibody (25 μg/mL). Nontransfected MCs are also exposed to medium containing recombinant human MCP-1 (10 ng/mL) or recombinant human TGF-1 (2 ng/mL). At 24 h after the media change, cells are harvested and the conditioned culture media are collected[2].

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

    Animal Administration
    [3]

    Rats[3]
    CCR2 antagonist RS102895 is dissolved in DMSO. Rats receive daily intrathecal injection of either RS102895 (3 g/L) 10 μL or 10 % DMSO 10 μL between 9 and 20 days after operation. All rats are randomLy divided into five groups (n = 10 per group): Sham group, Sham + RS102895 group, BCP group, BCP + RS102895 group, and BCP + DMSO group. Rats are sacrificed 20 days after operation and the tissue samples from the L4-L5 spinal cord segments are rapidly removed and immediately frozen in liquid nitrogen and stored at −80°C until use for RT-PCR and Western blot[3].

    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, 6 months; -20°C, 1 month (protect from light)。-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
    Ethanol / DMSO 1 mM 2.5615 mL 12.8074 mL 25.6148 mL 64.0369 mL
    5 mM 0.5123 mL 2.5615 mL 5.1230 mL 12.8074 mL
    10 mM 0.2561 mL 1.2807 mL 2.5615 mL 6.4037 mL
    15 mM 0.1708 mL 0.8538 mL 1.7077 mL 4.2691 mL
    20 mM 0.1281 mL 0.6404 mL 1.2807 mL 3.2018 mL
    25 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5615 mL
    30 mM 0.0854 mL 0.4269 mL 0.8538 mL 2.1346 mL
    40 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6009 mL
    50 mM 0.0512 mL 0.2561 mL 0.5123 mL 1.2807 mL
    60 mM 0.0427 mL 0.2135 mL 0.4269 mL 1.0673 mL
    80 mM 0.0320 mL 0.1601 mL 0.3202 mL 0.8005 mL
    100 mM 0.0256 mL 0.1281 mL 0.2561 mL 0.6404 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:
    RS102895
    目录号:
    HY-18611A
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