2. GPCR/G Protein Neuronal Signaling Anti-infection
  3. Neurokinin Receptor Bacterial HIV Antibiotic
  4. Aprepitant

Aprepitant  (Synonyms: 阿瑞匹坦; MK-0869; MK-869; L-754030)

目录号: HY-10052 纯度: 99.91%
COA 产品使用指南

摩尔计算器

Aprepitant (MK-0869) 是选择性和高亲和力的神经激肽1受体拮抗剂，Kd 值为86 pM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Aprepitant Chemical Structure

Aprepitant Chemical Structure

CAS No. : 170729-80-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥776
In-stock
1 mg ￥300
In-stock
5 mg ￥660
In-stock
10 mg ￥920
In-stock
50 mg ￥3300
In-stock
100 mg ￥4500
In-stock
200 mg 现货 询价
500 mg   询价  
1 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Aprepitant:

Aprepitant 相关抗体

Top Publications Citing Use of Products

    Aprepitant purchased from MCE. Usage Cited in: Research Square Print. 2023 Mar 2.

    Aprepitant (10 mg/kg; i.p.; every 2 days for 21 days) remarkably reduces the volume and weight of mice intrahepatic cholangiocarcinoma (iCCA) xenograft tumors without affecting the body weight of nude mice.

    查看 Neurokinin Receptor 亚型特异性产品:

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    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Aprepitant (MK-0869) is a selective and high-affinity neurokinin 1 receptor antagonist with a Kd of 86 pM.

    IC50 & Target

    Kd: 86 pM (Neurokinin 1 receptor)[1]
    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    18.3 μM
    Compound: Aprepitant
    Anti-cancer activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Anti-cancer activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34236855]
    A549 IC50
    18.3 μM
    Compound: Aprepitant
    Anti-cancer activity against human A549 cells incubated for 96 hrs by Resazurin assay
    Anti-cancer activity against human A549 cells incubated for 96 hrs by Resazurin assay
    		[PMID: 34236855]
    HEK293 IC50
    0.09 nM
    Compound: 1
    Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method
    Displacement of [125I]-substance P from gerbil NK1 receptor expressed in HEK293 cell membranes incubated for 30 mins by liquid scintillation counting method
    		[PMID: 26048800]
    MRC5 IC50
    28.9 μM
    Compound: Aprepitant
    Anti-cancer activity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    Anti-cancer activity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay
    		[PMID: 34236855]
    体外研究
    (In Vitro)

    Aprepitant decreases the metabolic activity with an estimated IC50 value of 20 µM. Aprepitant induces cell-growth inhibition and G1 cell-cycle arrest. Aprepitant significantly induces apoptosis in Nalm-6 cells, and the apoptosis is mediated through caspase-3 activation. Aprepitant (20 µM) induces p53 accumulation and expression of pro-apoptotic p53 target genes[2]. Aprepitant (1, 5, 10 µM) inhibits HIV infection in MDM from both depressed and not depressed HIV negative individuals ex vivo in a dose-dependent manner. IC90 value of aprepitant is equivalent to 10 μM, and the IC50 value is about 5 μM[4].

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

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

    Aprepitant prevents the increase of NK-1R expression induced by in vivo NHP infection with B. burgdorferi. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 protein levels in the CSF of NHPs. Aprepitant treatment prevents B. burgdorferi-induced increases in CCL2 and CXCL13 mRNA expression in the dorsal root ganglia of NHPs, prevents B. burgdorferi-induced increases in CCL2, CXCL13, IL-17A, and IL-6 mRNA expression in the spinal cord of NHPs. Aprepitant treatment attenuates B. burgdorferi infection-induced reductions in astrocyte activity/numbers[1]. Aprepitant (10 mg/kg, i.p.) significantly attenuates the CPP expression and locomotor activation produced by AMPH and cocaine in mice. Aprepitant does not induce significant CPP or conditioned place aversion or locomotor activation or suppression[3]. Aprepitant (125 mg/day, p.o.) results in 1 log reduction in plasma levels of viral RNA as compared to non-treated controls[4].

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

    534.43

    Formula

    C23H21F7N4O3
    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    阿瑞匹坦；阿瑞吡坦；阿瑞比坦
    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, 1 year; -20°C, 6 months (protect from light)

    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (187.12 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 1.8712 mL 9.3558 mL 18.7115 mL
    5 mM 0.3742 mL 1.8712 mL 3.7423 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, 1 year; -20°C, 6 months (protect from light)。-80°C储存时，请在1年内使用， -20°C储存时，请在6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： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.68 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。

      以 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 (4.68 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。

      以 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，请直接配制工作液。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： Corn Oil

      Solubility: 10 mg/mL (18.71 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

    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）。

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

    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: 99.91%

    COA (289 KB) LCMS (87 KB)

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

    The inhibitory effect of aprepitant on metabolic activity of Nalm-6 cells is assessed by uptake of thiazolyl blue tetrazolium bromide (MTT) by viable cells. Cells are plated onto 96-well plates at a density of 5000 cells/well. After treatment with aprepitant at 5, 10, 15, 20 and 30 µM for 24, 36 and 48 h, the cells are further incubated with 100 μL of MTT (0.5 mg/mL) at 37°C for 3 h. Untreated cells are defined as the control group. Following solubilization of precipitated formazan with 100 μL of DMSO, the optical densitometry is measured with an ELISA reader at a wavelength of 578 nm.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Fifteen rhesus macaques are anesthetized and inoculated intrathecally with 1×108 live spirochetes into the cisterna magna, whereas five rhesus macaques are left uninfected and receive 1 mL of RPMI 1640 medium after removing an equivalent volume of CSF. The establishment of in vivo B. burgdorferi infection is confirmed by positive culture from at least necropsy tissue sample. The first set of animals are studied for 2 weeks and included two control animals (one of which is treated with aprepitant), two infected and untreated animals, and two infected animals that are treated with aprepitant. The second set of animals are studied for 4 weeks and included three control animals (one of which is treated with aprepitant), five infected and untreated animals, and four infected animals treated with aprepitant. Animals receive an average dose of aprepitant of 28 ± 6 mg/kg per day p.o. daily, and drug treatments are started 2 days before inoculation. These doses are consistent with standard veterinary regimens for the chosen drugs in NHP, and the 4-week duration of the study precludes the development of neural pathology that occurs at 8 weeks following B. burgdorferi infection.

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

    Aprepitant 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, 1 year; -20°C, 6 months (protect from light)。-80°C储存时，请在1年内使用， -20°C储存时，请在6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
    DMSO 1 mM 1.8712 mL 9.3558 mL 18.7115 mL 46.7788 mL
    5 mM 0.3742 mL 1.8712 mL 3.7423 mL 9.3558 mL
    10 mM 0.1871 mL 0.9356 mL 1.8712 mL 4.6779 mL
    15 mM 0.1247 mL 0.6237 mL 1.2474 mL 3.1186 mL
    20 mM 0.0936 mL 0.4678 mL 0.9356 mL 2.3389 mL
    25 mM 0.0748 mL 0.3742 mL 0.7485 mL 1.8712 mL
    30 mM 0.0624 mL 0.3119 mL 0.6237 mL 1.5593 mL
    40 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1695 mL
    50 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9356 mL
    60 mM 0.0312 mL 0.1559 mL 0.3119 mL 0.7796 mL
    80 mM 0.0234 mL 0.1169 mL 0.2339 mL 0.5847 mL
    100 mM 0.0187 mL 0.0936 mL 0.1871 mL 0.4678 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:

    Aprepitant170729-80-3MK-0869 MK-869 L-754030阿瑞匹坦阿瑞吡坦阿瑞比坦MK0869MK 0869MK869MK 869MK-869L754030L 754030L-754030Neurokinin ReceptorBacterialHIVAntibioticNK receptorTachykinin receptorHuman immunodeficiency virusInhibitorinhibitorinhibit

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