2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. INCB3344

INCB3344 是一种有效的 CCR2 拮抗剂，拮抗结合活性时，IC50 为 5.1 nM (hCCR2) 和 9.5 nM (mCCR2)，拮抗趋化活性时，IC50 为 3.8 nM (hCCR2) 和 7.8 nM (mCCR2)。

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INCB3344 Chemical Structure

INCB3344 Chemical Structure

CAS No. : 1262238-11-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2033
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1 mg ￥727
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5 mg ￥1600
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10 mg ￥2600
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Customer Review

Other Forms of INCB3344:

INCB3344 相关抗体

Top Publications Citing Use of Products

    INCB3344 purchased from MCE. Usage Cited in: Oncotarget. 2018 Jul 13;9(76):34213-34228.  [Abstract]

    The use of INCB 3344 leads to significant reduction of HBsAgs.

    INCB3344 purchased from MCE. Usage Cited in: Hum Vaccin Immunother. 2017 Dec 2;13(12):2872-2882.  [Abstract]

    Blockage of Ly6Chi monocytes abrogates HBV clearance by the 3 × GM-CSF+VACCINE. The AAV8–1.3HBV infected mice are treated with CCR2 antagonist (INCB 3344, 30 mg/kg) by intraperitoneal injection one hour before GM-CSF, repeated at day 2, 3, and 4. The CD11b+Ly6Chi monocytes are measured 12 hours after the fourth INCB 3344 administration.

    INCB3344 purchased from MCE. Usage Cited in: Hypertension. 2012 Nov;60(5):1207-12.  [Abstract]

    Effect of intervention with a CCR2 antagonist, INCB3344 (30 mg/kg per day), on Deoxycorticosterone acetate/salt-induced increases in expression of CCR2 (A), CCL2 (B), CCL7 (C), CCL8 (D), and CCL12 (E) in aortas of mice.

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    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

    IC50 & Target

    hCCR2

    5.1 nM (IC50)

    mCCR2

    9.5 nM (IC50)

    体外研究
    (In Vitro)

    INCB3344 is a potent antagonist towards rat and cynomolgus CCR2 as well, displaying IC50 values of 7.3 and 16 nM in binding antagonism and 2.7 and 6.2 nM in antagonism of chemotaxis activity, respectively. INCB3344 is a selective hCCR2 antagonist, exhibiting IC50 values of more than 1 μM against a panel of >50 ion channels, transporters, chemokine receptors and other selected GPCRs. It is also a selective mCCR2 antagonist, showing IC50 values of >1 μM and >3 μM against murine CCR1 and murine CCR5, respectively, the two most homologous chemokine receptors to mCCR2[1]. Characterization of the pharmacological activity of INCB3344 is first evaluated by testing its ability to inhibit CCL2 binding to CCR2 in a whole cell binding assay using a murine monocyte cell line, WEHI-274.1 and 125I-labeled mCCL2 as a tracer. The binding IC50 of INCB3344 in this assay is determined to be 10±5 nM, and inhibition of >90% binding is observed at a concentration of 90 nM[2].

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

    INCB3344 相关抗体:
    体内研究
    (In Vivo)

    When administered intravenously to CD-1 mice, INCB3344 exhibits a high clearance and a moderate volume of distribution, resulting in a short half life of 1 h. Despite its high clearance, however, good oral exposure is achieved, with an AUC at 2664 nM h at a dose of 10 mg/kg. The oral bioavailability is 47%. By comparison, slightly better oral exposure (AUC=3888 nM h) is obtained when administered orally to Balb/c mice at the same dose. This PK property, couple with its potent anti-mCCR2 activity and good selectivity, makes this compound suitable for model studies in rodents[1]. INCB3344 prevents Deoxycorticosterone acetate/salt-induced changes in vascular expression of CCR2. In a separate series of experiments, CCR2 expression is elevated (≈1.5-fold higher) in aortas from mice that receive INCB3344 from days 7 to 21 of the Deoxycorticosterone acetate/salt treatment period compare with sham animals; however, this level of CCR2 expression is significantly lower than that observed in the vehicle-treated group (P<0.05, n=6). Likewise, increased expression of its receptor ligand CCL2 in Deoxycorticosterone acetate/salt-treated mice is blunted in mice receiving INCB3344 (P<0.05, n=6). By contrast, levels of CCL7, CCL8, and CCL12 are elevated to similar extents in Deoxycorticosterone acetate/salt-treated mice receiving vehicle or INCB3344[3].

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

    577.59

    Formula

    C29H34F3N3O6
    CAS 号
    性状

    固体

    颜色

    White to yellow

    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 220 mg/mL (380.89 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 : 100 mg/mL (173.13 mM; 超声助溶)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.7313 mL 8.6567 mL 17.3133 mL
    5 mM 0.3463 mL 1.7313 mL 3.4627 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。-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    95% (20% SBE-β-CD in Saline)

      Solubility: 6 mg/mL (10.39 mM); 澄清溶液; 超声助溶

    • 方案 二

      请依序添加每种溶剂： 5% DMSO    95% Corn Oil

      Solubility: 6 mg/mL (10.39 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: 99.73%

    COA (191 KB) LCMS (114 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    WEHI-274.1 cells (5×105) in RPMI 1640 (VWR) with or without various concentrations of INCB3344 in RPMI 1640 are loaded in the wells on top of an 8-μm polycarbonate filter in a 96-well-modified Boyden chamber. Beneath the filter, 30 nM mCCL2 with or without INCB3344 or media is placed in a corresponding 96-well plate. The sealed chambers are incubated for 45 min at 37°C, 5% CO2. Filters are washed, stained with Wright-Giemsa, and the number of cells that migrate toward mCCL2 in the bottom chamber counted by microscopy. The ability of INCB3344 to antagonize CCR2-mediated chemotaxis is reported as the inhibitor concentration required for IC50 values of specific migration to mCCL2. Specific migration is defined as the total migration minus the background migration. A similar assay is used to determine the impact of INCB3344 on CCR1-mediated chemotaxis of WEHI-274.1 cells, by using mouse MIP-1α as a ligand. In addition C5a, FMLP and RANTES are similarly tested in the presence of INCB3344 for migration of WEHI-274.1 cells. For the studies on the impact of INCB3344 on CCR5-mediated chemotaxis, murine T cells are used as the cell system with mouse MIP-1β as the ligand[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    In a subset of experiments, Deoxycorticosterone acetate/salt-treated mice are further randomly assigned to receive the CCR2 antagonist, INCB3344 (30 mg/kg per day; Haoyuan Chemexpress Co Ltd) or vehicle (10% DMSO/0.9% carboxymethylcellulose) via daily intraperitoneal injections commencing 10 days after induction of hypertension and continuing until the end of the 21-day treatment period. The normotensive control group for these experiments consist of sham-treated mice that receive vehicle from days 10 to 21.
    Rats[4]
    Adult male Sprague-Dawley rats (200-250 g) are used. 1 μg of CCL2 and/or 1 mM of INCB3344 is administered intrathecally between L5 and L6 vertebrae. Animals are tested once at 30, 60, 90, 120, and 240 min following drug administration. The percentage of maximal potential effect (MPE) is calculated for every time point.

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

    INCB3344 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, 6 months; -20°C, 1 month。-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 1.7313 mL 8.6567 mL 17.3133 mL 43.2833 mL
    5 mM 0.3463 mL 1.7313 mL 3.4627 mL 8.6567 mL
    10 mM 0.1731 mL 0.8657 mL 1.7313 mL 4.3283 mL
    15 mM 0.1154 mL 0.5771 mL 1.1542 mL 2.8856 mL
    20 mM 0.0866 mL 0.4328 mL 0.8657 mL 2.1642 mL
    25 mM 0.0693 mL 0.3463 mL 0.6925 mL 1.7313 mL
    30 mM 0.0577 mL 0.2886 mL 0.5771 mL 1.4428 mL
    40 mM 0.0433 mL 0.2164 mL 0.4328 mL 1.0821 mL
    50 mM 0.0346 mL 0.1731 mL 0.3463 mL 0.8657 mL
    60 mM 0.0289 mL 0.1443 mL 0.2886 mL 0.7214 mL
    80 mM 0.0216 mL 0.1082 mL 0.2164 mL 0.5410 mL
    100 mM 0.0173 mL 0.0866 mL 0.1731 mL 0.4328 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:

    INCB33441262238-11-8INCB 3344INCB-3344CCRCC chemokine receptorInhibitorinhibitorinhibit

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