萊莫維韋|T5396|TargetMol

價格	￥725	￥1060	￥1930
包裝	1mg	2mg	5mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:萊莫維韋	英文名稱:Letermovir
CAS:917389-32-3	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.93%	產(chǎn)品類別: 抑制劑
貨號: T5396

Product Introduction

Bioactivity

名稱	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.
細胞實驗	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].
動物實驗	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].
體外活性	Letermovir的抑制效力在EC50s方面超過了ganciclovir (GCV) 400倍以上（平均約4.5 nM對比約2 μM），在EC90值方面超過了2000倍以上（平均約6.1 nM對比約14.5 μM）。在抗病毒測試期間，當(dāng)Letermovir濃度<33 μM時，NHDF單層細胞未顯示出在顯微鏡下可見的細胞毒性效應(yīng)[1]。Letermovir對人類巨細胞病毒具有顯著的特異性，因為在測試的其他所有皰疹病毒中均未注意到顯著活性[2]。
體內(nèi)活性	Letermovir治療導(dǎo)致移植細胞內(nèi)HCMV滴度與安慰劑對照組相比呈劑量依賴性降低，使用的是小鼠異種移植模型。統(tǒng)計分析顯示，Letermovir的10-, 30-, 和100-mg/kg/日治療組以及100-mg/kg/日VGCV對照組均顯著抗病毒效果[1]。與安慰劑相比，letermovir的預(yù)防失敗率為60 mg/日劑量時為48%，120 mg劑量時為32%，240 mg劑量時為29%。Kaplan-Meier預(yù)防失敗的起始時間曲線對于每日240 mg劑量的letermovir與安慰劑的比較顯示出顯著差異[3]。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : 2 mg/mL DMSO : 70 mg/mL (122.26 mM)
關(guān)鍵字	Cytomegalovirus \| MK 8828 \| AIC-246 \| Inhibitor \| CMV \| MK8828 \| Letermovir \| inhibit \| AIC 246
相關(guān)產(chǎn)品	Resiquimod \| RO8191 \| Honokiol \| Grazoprevir \| Artemisinin \| EIDD-1931 \| Methyl 2-amino-5-bromobenzoate \| Deferiprone \| HCV-IN-30 \| Ribavirin \| HCV-IN-29 \| Sofosbuvir
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| EMA 上市藥物庫 \| FDA 上市藥物庫 \| 抗病毒庫 \| 藥物功能重定位化合物庫

關(guān)鍵字：萊莫維韋|||MK-8828|||AIC246|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個性化定制合成；從對明確靶點的分子篩選到對明確分子的多靶點篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國市場五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊資本	566.2651萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場三路28號4樓

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