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Letermovir

产品编号 T5396 CAS 917389-32-3

别名: AIC246, MK-8828, 莱莫维韦

Letermovir (AIC246) 是一种新型抗 CMV 抑制剂，靶向病毒末端酶，抑制其活性。

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Letermovir, CAS 917389-32-3

规格	价格/CNY	货期
1 mg	￥ 725	现货
2 mg	￥ 1,060	现货
5 mg	￥ 1,930	现货
10 mg	￥ 2,930	现货
25 mg	￥ 4,680	现货
50 mg	￥ 6,320	现货
100 mg	￥ 8,770	现货
500 mg	￥ 17,500	待询
1 mL * 10 mM (in DMSO)	￥ 2,380	现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Letermovir (AIC246) (AIC246) is a novel anti-CMV compound (EC50: about 5 nM in fibroblast cells). It targets the pUL56 subunit of the viral terminase complex.
靶点活性	HCMV:~5 nM (in fibroblast cells)
体外活性	The inhibitory potency of AIC246 surpasses ganciclovir (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). NHDF monolayers showed no microscopically apparent cytotoxic effects at AIC246 concentrations of <33 μM when observed during antiviral assays [1]. AIC246 is remarkably specific for human cytomegaloviruses since no significant activity was noted against any other herpesvirus tested. The EC50s obtained for RCMV and MCMC indicated that no (RCMV) or only a very low-level (MCMV, 4.51 μM) AIC246 sensitivity could be detected even for rodent cytomegaloviruses [2].
体内活性	AIC246 treatment led 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. Statistical analysis revealed significant antiviral effects for the 10-, 30-, and 100-mg/kg/day treatment groups of AIC246 as well as for the 100-mg/kg/day VGCV control group [1]. The incidence of prophylaxis failure with letermovir, as compared with placebo, was 48% versus 64% at a daily letermovir dose of 60 mg, 32% at a dose of 120 mg, and 29% at a dose of 240 mg. Kaplan-Meier time-to-onset profiles for prophylaxis failure showed a significant difference in the comparison of letermovir at a dose of 240 mg per day with placebo [3].
细胞实验	Briefly, 96-well microtiter plates were seeded with 1.5 × 10^4 cells/well and incubated overnight. Drugs were added to the wells in 3-fold serial dilutions starting from 0.33 mM (the DMSO concentration was kept constant at 0.66% throughout the whole plate). After a 7-day incubation period, alamarBlue solution was added to each well and the fluorescence signal was measured using a SpectraFluor Plus fluorescence reader. The relative fluorescence units of treated wells were expressed as percentages of untreated cell control wells and plotted against the logarithm of drug concentrations. Drug concentrations reducing cell viability by 50% (CC50s) were determined from dose-response curves. The assays were performed at least three times with duplicate samples. CC50 values were used to calculate the selectivity index (SI = CC50/EC50) for individual substances [1].
动物实验	Briefly, Gelfoam hemostyptic gelatin devices were cut aseptically into 1-cm2 pieces. These implants were soaked in NHDF cell culture growth medium (GM), and sponges were brought to 37°C in a CO2 incubator. NHDF cells were infected with cell-free HCMV strain Davis at an MOI of 0.03. After 4 h, cells were collected by trypsinization followed by centrifugation at room temperature for 10 min at 800 × g. Cells were resuspended in GM and counted using a hemocytometer. Each Gelfoam implant was seeded with a suspension of 1 × 10^6 infected cells by pipetting the cells onto the sponges. Human cells were allowed to adhere to the collagen sponges for at least 3 to 4 h at 37°C. To enhance vascularization of the implant, 250 ng recombinant human basic fibroblast growth factor was pipetted onto each implant 1 h prior to transplantation. Mice (18 to 25 g body weight) were anesthetized, and the Gelfoam sponges were implanted subcutaneously in the dorsoscapular area. After transplantation, mice were randomized and grouped in ～10 animals per treatment group. Starting 4 h after transplantation, mice were treated once daily with the indicated compounds for nine consecutive days. Drugs were applied per os by oral gavage. Total administration volume was 10 ml/kg. Mice were sacrificed after 9 days of treatment, and the Gelfoam implants were removed and digested with collagenase at 37°C. After 2 to 3 h, human cells were recovered by centrifugation and resuspended in GM. Subsequently, the isolated cell suspensions were serially diluted and mixed with uninfected NHDF indicator cells and PFU were determined by plaque assays. Virus titers determined from isolated cells are given as PFU/ml [1].

别名	AIC246, MK-8828, 莱莫维韦
分子量	572.55
分子式	C29H28F4N4O4
CAS No.	917389-32-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: 2 mg/mL

DMSO: 70 mg/mL (122.26 mM)

溶液配制表

可选溶剂	浓度体积质量	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
	20 mM	0.0873 mL	0.4366 mL	0.8733 mL	2.1832 mL
	50 mM	0.0349 mL	0.1747 mL	0.3493 mL	0.8733 mL
	100 mM	0.0175 mL	0.0873 mL	0.1747 mL	0.4366 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Lischka P, et al. In vitro and in vivo activities of the novel anticytomegalovirus compound AIC246. Antimicrob Agents Chemother. 2010 Mar;54(3):1290-7. 2. Marschall M, et al. In vitro evaluation of the activities of the novel anticytomegalovirus compound AIC246 (letermovir) against herpesviruses and other human pathogenic viruses. Antimicrob Agents Chemother. 2012 Feb;56(2):1135-7. 3. Chemaly RF, et al. Letermovir for cytomegalovirus prophylaxis in hematopoietic-cell transplantation.N Engl J Med. 2014 May 8;370(19):1781-9.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Letermovir 917389-32-3 Microbiology/Virology Others Proteases/Proteasome HCV Protease AIC246 MK-8828 Cytomegalovirus MK 8828 AIC-246 Inhibitor CMV MK8828 inhibit 莱莫维韦 AIC 246 inhibitor

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Letermovir

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords