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  • 莱莫维韦|T5396|TargetMol

莱莫维韦|T5396|TargetMol

Letermovir
917389-32-3
725 1mg 起订
1060 2mg 起订
1930 5mg 起订
上海 更新日期:2026-01-06

TargetMol中国(陶术生物)

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产品详情:

中文名称:
莱莫维韦
英文名称:
Letermovir
CAS号:
917389-32-3
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
产品类别:
抑制剂
货号:
T5396

Product Introduction

Bioactivity

名称Letermovir
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.
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].
体外活性Letermovir的抑制效力在EC50s方面超过了ganciclovir (GCV) 400倍以上(平均约4.5 nM对比约2 μM),在EC90值方面超过了2000倍以上(平均约6.1 nM对比约14.5 μM)。在抗病毒测试期间,当Letermovir浓度<33 μM时,NHDF单层细胞未显示出在显微镜下可见的细胞毒性效应[1]。Letermovir对人类巨细胞病毒具有显著的特异性,因为在测试的其他所有疱疹病毒中均未注意到显著活性[2]。
体内活性Letermovir治疗导致移植细胞内HCMV滴度与安慰剂对照组相比呈剂量依赖性降低,使用的是小鼠异种移植模型。统计分析显示,Letermovir的10-, 30-, 和100-mg/kg/日治疗组以及100-mg/kg/日VGCV对照组均显著抗病毒效果[1]。与安慰剂相比,letermovir的预防失败率为60 mg/日剂量时为48%,120 mg剂量时为32%,240 mg剂量时为29%。Kaplan-Meier预防失败的起始时间曲线对于每日240 mg剂量的letermovir与安慰剂的比较显示出显著差异[3]。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度Ethanol : 2 mg/mL (3.49 mM), Sonication is recommended.
DMSO : 70 mg/mL (122.26 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.49 mM), Sonication is recommended.
关键字MK8828 | MK 8828 | Letermovir | Inhibitor | inhibit | HCVProtease | HCV Protease | HCMV | Cytomegalovirus | CMV | AIC-246 | AIC 246
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莱莫维韦|||MK-8828|||AIC246|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起,为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部,化学事业部,生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应;从商业化产品销售到个性化定制合成;从对明确靶点的分子筛选到对明确分子的多靶点筛选,从高通量筛选到化学结构优化,我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘,我们已成为筛选化合物领域优秀的供应商,为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (13年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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