1. GPCR/G Protein
  2. LPL Receptor
  3. AM966

AM966 是一种高亲和性的选择性LPA1-拮抗剂,抑制LPA-刺激的细胞内钙释放,IC50 为 17 nM。

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AM966 Chemical Structure

AM966 Chemical Structure

CAS No. : 1228690-19-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1512
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2 mg ¥990
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5 mg ¥1400
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10 mg ¥2150
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50 mg ¥3400
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100 mg ¥5400
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Top Publications Citing Use of Products

    AM966 purchased from MCE. Usage Cited in: J Biol Chem. 2016 Dec 30;291(53):27364-27370.  [Abstract]

    Effect of LPAR antagonists on ERK1/2 phosphorylation and FRS2 phosphorylation evoked by either amitriptyline (A) or LPA (B).

    AM966 purchased from MCE. Usage Cited in: J Pharmacol Exp Ther. 2016 Nov;359(2):340-353.  [Abstract]

    Concentration-dependent effects of LPA receptor antagonists on antidepressant- and LPA-induced ERK1/2 phosphorylation in C6 glioma cells. Cells are pre-incubated with either vehicle or the indicated concentrations of AM966 for 10 min and then exposed to either vehicle or 1 μM LPA (A), 15 μM Amitriptyline (C) or 5 μM Mianserin (E) for 10 min.

    AM966 purchased from MCE. Usage Cited in: Biochem Pharmacol. 2015 Jun 15;95(4):311-23.  [Abstract]

    CHO-K1 cells express LPA1 receptors coupled to ERK1/2 phosphorylation. Inhibition of LPA-induced phospho-ERK1/2 by AM966. Cells are pre-incubated with either vehicle or the indicated concentrations of AM966 for 30 min and then treated with LPA (300 nM) for 15 min. Values are expressed as percent of p-ERK stimulation elicited by LPA in the absence of antagonist and are the mean ± SEM of three experiments.

    AM966 purchased from MCE. Usage Cited in: College of Pharmacy. Washington State University. 2015 May.

    Effects of LPAR antagonists on growth factor-induced phosphorylation of ERK in DU145 cells. Serum starved DU145 cells are incubated with 10 μM LPA, with or without either 100 nM AM966 or 10 μM Ki16425 for 10 minutes. Whole-cell extracts, equalized for protein, are immunoblotted for phospho-ERK (pERK) and for actin (loading control).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    AM966 is a high affinity, selective, oral LPA1-antagonist, inhibits LPA-stimulated intracellular calcium release (IC50=17 nM).

    IC50 & Target

    LPA1[1]

    体外研究
    (In Vitro)

    AM966 是一种有效的、选择性的、口服生物可利用的 LPA1 受体拮抗剂。AM966 抑制 LPA1 介导的人 A2058 黑色素瘤细胞 (IC50=138±43 nM)、IMR-90 人肺成纤维细胞 (IC50=182±86 nM) 和 CHO mLPA1 细胞 (IC50=469±54 nM)[1]。LPA 诱导的 ERK1/2 激活被 AM966 (100 nM) 完全阻断,它选择性地拮抗 LPA1 而不是 LPA2-5,IC50 值为 3.8±0.4 nM。用 AM966 (100 nM) 预处理完全阻断米安色林诱导的 ERK1/2 磷酸化[2]

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

    体内研究
    (In Vivo)

    AM966 (30 mg/kg,BID) 在 3 天 Bleomycin (HY-108345) 模型中减少血管渗漏、炎症和肺损伤和炎症。AM966 在 Bleomycin 肺损伤后 14 天抑制肺纤维化,维持小鼠体重并减少肺部炎症。在为期 14 天的 Bleomycin 研究中,AM966 减少了血管渗漏、组织损伤和促纤维化细胞因子的产生。与 Pirfenidone (HY-B0673) 相比,AM966 在 14 天的 Bleomycin 模型中表现出更高的功效。AM966 可降低 Bleomycin 损伤后晚期的死亡率和纤维化[1]

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

    分子量

    490.93

    Formula

    C27H23ClN2O5

    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
    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 (203.70 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.0370 mL 10.1848 mL 20.3695 mL
    5 mM 0.4074 mL 2.0370 mL 4.0739 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 (5.09 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      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 (5.09 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: 10 mg/mL (20.37 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
    参考文献
    Cell Assay
    [2]

    CHO-K1 cells are grown to 80% confluency in 12-well plates, serum-starved for 24 h and incubated in serum-free medium with AM966. After 21 h, [3H]thymidine (0.5 μCi/well) is added and the incubation is continued for 3 h. The medium is then removed, and the cells are placed on ice and washed twice with 1 mL of ice-cold PBS containing 5% trichloroacetic acid. Cells are solubilized and [3H]thymidine incorporation is determined by liquid scintillation counting. Assays are performed in triplicate[2].

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

    Animal Administration
    [1]

    Mice[1]
    The oral exposure of AM966 is determined in fasted mice. Animals received AM966 (10 mg/kg) in vehicle (water) by oral gavage and are then killed by CO2 inhalation at 1, 2, 4, 8 and 24 h post dose (n=2 animals per time point for each test compound). Blood (approximately 300 µL) is collected via cardiac puncture into EDTA-containing tubes and centrifuged at 1450×g for 10 min. The plasma is removed and analysed for AM966 content by liquid chromatography-mass spectrometry (LCMS). Briefly, known amounts of AM966 are added to thawed mouse plasma to yield a concentration range from 0.8 to 4000 ng/mL. Mouse plasma samples are precipitated using acetonitrile (1:4, v:v) containing the internal standard buspirone. A 10 µL aliquot of the analyte mixture is injected using a Leap PAL autosampler. Analyses are performed using an Agilent Zorbax SB-C8 column (2.1×50 mm; 5 µm) linked to a Shimadzu LC-10AD VP with SCL-10A VP system controller. Tandem mass spectrometric detection is carried out on a PE Sciex API3200 in the positive ion mode (ESI) by multiple reaction monitoring. The calibration curves are constructed by plotting the peak-area ratio of analysed peaks against known concentrations. The lower limit of quantitation is 0.8 ng/mL. The data are subjected to linear regression analysis with 1/x2weighting.

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

    参考文献

    AM966 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 2.0370 mL 10.1848 mL 20.3695 mL 50.9238 mL
    5 mM 0.4074 mL 2.0370 mL 4.0739 mL 10.1848 mL
    10 mM 0.2037 mL 1.0185 mL 2.0370 mL 5.0924 mL
    15 mM 0.1358 mL 0.6790 mL 1.3580 mL 3.3949 mL
    20 mM 0.1018 mL 0.5092 mL 1.0185 mL 2.5462 mL
    25 mM 0.0815 mL 0.4074 mL 0.8148 mL 2.0370 mL
    30 mM 0.0679 mL 0.3395 mL 0.6790 mL 1.6975 mL
    40 mM 0.0509 mL 0.2546 mL 0.5092 mL 1.2731 mL
    50 mM 0.0407 mL 0.2037 mL 0.4074 mL 1.0185 mL
    60 mM 0.0339 mL 0.1697 mL 0.3395 mL 0.8487 mL
    80 mM 0.0255 mL 0.1273 mL 0.2546 mL 0.6365 mL
    100 mM 0.0204 mL 0.1018 mL 0.2037 mL 0.5092 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:
    HY-15277
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