2. Anti-infection
  3. CMV
  4. Letermovir

Letermovir  (Synonyms: 莱莫维韦; AIC246; MK-8228)

目录号: HY-15233 纯度: 99.96%
COA 产品使用指南

摩尔计算器

Letermovir (AIC246) 是一种有效的 CMV 抑制剂，以病毒末端酶为靶目标，抑制其活性。

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Letermovir Chemical Structure

Letermovir Chemical Structure

CAS No. : 917389-32-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2929
In-stock
1 mg ￥906
In-stock
5 mg ￥2325
In-stock
10 mg ￥3534
In-stock
25 mg ￥5650
In-stock
50 mg 现货 询价
100 mg 现货 询价
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Letermovir:

Letermovir 相关抗体

Top Publications Citing Use of Products

    Letermovir purchased from MCE. Usage Cited in: Eur J Pharm Sci. 2019 Jan 15;127:29-37.  [Abstract]

    Viral reporter GFP expression after inoculation and compound treatment. Infected cells treated with DMSO control, BIO, Ganciclovir (GCV) or Letermovir (LTR)

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Letermovir (AIC246) is a potent inhibitor of CMV, which targets the viral terminase complex and remains active against virus resistant to DNA polymerase inhibitors.

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    HEL 299 EC50
    0.0035 μM
    Compound: AIC246
    Antiviral activity against human cytomegalovirus infected in HEL299 cells after 7 days by GFP-based fluorescent reduction assay
    Antiviral activity against human cytomegalovirus infected in HEL299 cells after 7 days by GFP-based fluorescent reduction assay
    		[PMID: 20047911]
    HEL 299 CC50
    63 μM
    Compound: AIC246
    Cytotoxicity against HEL299 cells infected with human cytomegalovirus after 7 days by alamar blue assay
    Cytotoxicity against HEL299 cells infected with human cytomegalovirus after 7 days by alamar blue assay
    		[PMID: 20047911]
    HS27 EC50
    0.0056 μM
    Compound: AIC246
    Antiviral activity against human cytomegalovirus infected in human HS27 cells after 7 days by GFP-based fluorescent reduction assay
    Antiviral activity against human cytomegalovirus infected in human HS27 cells after 7 days by GFP-based fluorescent reduction assay
    		[PMID: 20047911]
    HS27 CC50
    107 μM
    Compound: AIC246
    Cytotoxicity against human HS27 cells infected with human cytomegalovirus after 7 days by alamar blue assay
    Cytotoxicity against human HS27 cells infected with human cytomegalovirus after 7 days by alamar blue assay
    		[PMID: 20047911]
    MRC5 EC50
    0.0045 μM
    Compound: AIC246
    Antiviral activity against human cytomegalovirus infected in human MRC5 cells after 7 days by GFP-based fluorescent reduction assay
    Antiviral activity against human cytomegalovirus infected in human MRC5 cells after 7 days by GFP-based fluorescent reduction assay
    		[PMID: 20047911]
    MRC5 CC50
    127 μM
    Compound: AIC246
    Cytotoxicity against human MRC5 cells infected with human cytomegalovirus after 7 days by alamar blue assay
    Cytotoxicity against human MRC5 cells infected with human cytomegalovirus after 7 days by alamar blue assay
    		[PMID: 20047911]
    NHDF CC50
    91 μM
    Compound: AIC246
    Cytotoxicity against NHDF infected with human cytomegalovirus after 7 days by alamar blue assay
    Cytotoxicity against NHDF infected with human cytomegalovirus after 7 days by alamar blue assay
    		[PMID: 20047911]
    体外研究
    (In Vitro)

    AIC246 has consistent antiviral efficacy, and there is remarkable selectivity of AIC246 for human cytomegaloviruses[1]. AD169 mutant strains and designated rAIC246-1 and rAIC246-2 are highly resistant to Letermovir (AIC246), with EC50s of 5.6 nM, 1.24 μM, 0.37 μM, respectively. Letermovir inhibits HCMV replication through a specific antiviral mechanism that involves the viral gene product UL56. Letermovir inhibits HCMV replication in cell culture by interfering with the proper cleavage/packaging of HCMV progeny DNA[2]. Letermovir inhibits the current gold standard GCV by more than 400-fold with respect to EC50s (mean, 4.5 nM versus 2 μM) and by more than 2,000-fold with respect to EC90 values (mean, 6.1 nM versus 14.5 μM)[3]. Letermovir in conbination with anti-HCMV drugs causes additive antiviral effects, but there is no interaction between letermovir and anti-HIV drugs[4].

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

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

    Letermovir (10-100 mg/kg/day, p.o.) leads to a dose-dependent reduction of the HCMV titer in transplanted cells compared to that of the placebo-treated control group using the mouse xenograft model[3].

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

    572.55

    Formula

    C29H28F4N4O4
    CAS 号
    性状

    固体

    颜色

    Off-white to yellow

    中文名称

    莱莫维韦
    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
    细胞实验： 

    DMSO 中的溶解度 : ≥ 100 mg/mL (174.66 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 1.7466 mL 8.7329 mL 17.4657 mL
    5 mM 0.3493 mL 1.7466 mL 3.4931 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

    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 (4.37 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.37 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 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      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

    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: 99.96%

    COA (291 KB) HNMR (293 KB) LCMS (93 KB)

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

    Briefly, 5×103 AD169-infected NHDF cells/well are seeded into the wells of 30 96-well microtiter plates. The infection is allowed to proceed under the exposure of 50 nM AIC246 (10×EC50) until a CPE developed in one or more of the compound-treated wells (indicative of resistant virus breakthrough). Noninfected and nontreated cells serve as controls on each plate. Mutant virus amplification is accomplwashed after cultures achieved maximum CPE by the passage of cell-free supernatant virus in the presence of 50 nM AIC246. The resultant AIC246-resistant progeny virus mutants are plaque purified three times by limiting dilutions in the presence of AIC246. The stability of resistance is tested by serially passaging plaque-purified viruses without selective pressure (8 to 10 times).

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

    Mice (18 to 25 g body weight) are anesthetized, and the Gelfoam sponges are implanted subcutaneously in the dorsoscapular area. After transplantation, mice are randomized and grouped in 10 animals per treatment group. Starting 4 h after transplantation, mice are treated once daily with letermovir for nine consecutive days. Drugs are applied per os by oral gavage. Total administration volume is 10 mL/kg. Mice are sacrificed after 9 days of treatment, and the Gelfoam implants are removed and digested with collagenase at 37°C. After 2 to 3 h, human cells are recovered by centrifugation and resuspended in GM. Subsequently, the isolated cell suspensions are serially diluted and mixed with uninfected NHDF indicator cells and PFU are determined by plaque assays as described above. Virus titers determined from isolated cells are given as PFU/mL.

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

    Letermovir 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 1.7466 mL 8.7329 mL 17.4657 mL 43.6643 mL
    5 mM 0.3493 mL 1.7466 mL 3.4931 mL 8.7329 mL
    10 mM 0.1747 mL 0.8733 mL 1.7466 mL 4.3664 mL
    15 mM 0.1164 mL 0.5822 mL 1.1644 mL 2.9110 mL
    20 mM 0.0873 mL 0.4366 mL 0.8733 mL 2.1832 mL
    25 mM 0.0699 mL 0.3493 mL 0.6986 mL 1.7466 mL
    30 mM 0.0582 mL 0.2911 mL 0.5822 mL 1.4555 mL
    40 mM 0.0437 mL 0.2183 mL 0.4366 mL 1.0916 mL
    50 mM 0.0349 mL 0.1747 mL 0.3493 mL 0.8733 mL
    60 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7277 mL
    80 mM 0.0218 mL 0.1092 mL 0.2183 mL 0.5458 mL
    100 mM 0.0175 mL 0.0873 mL 0.1747 mL 0.4366 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:

    Letermovir917389-32-3AIC246 MK-8228莱莫维韦AIC 246AIC-246MK8228MK 8228MK-8228CMVCytomegalovirusInhibitorinhibitorinhibit

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