達拉他韋|T6229|TargetMol

價格	￥223	￥497	￥756
包裝	1mg	5mg	10mg

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:達拉他韋	英文名稱:Daclatasvir
CAS:1009119-64-5	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: 99.81%	產(chǎn)品類別: 抑制劑
貨號: T6229

Product Introduction

Bioactivity

名稱	Daclatasvir
描述	Daclatasvir (EBP 883) (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.
細胞實驗	BMS-790052 is added to 96-well plates containing HCV replicon cells seeded approximately 12?hours before in 200 μL media.The cell plates are tested for replication activity and cytotoxicity after 72 hours of incubation. Cytotoxicity is measured with CellTiter-Blue, after which the media and dye are removed, plates are inverted and the remaining liquid is blotted with paper towels. Replication activity of the HCV genotype 1a cell lines is quantified using Renilla luciferase. 1× Renilla luciferase lysis buffer (30 μL) is added to each well and plates are incubated with gentle shaking for 15?min. Renilla luciferase substrate (40 μL) is then added and the signals are detected using a Top Count luminometer set for light emission quantification. One hundred per cent activity is calculated for each cell line for the DMSO-only wells; percentage activity is calculated for each concentration of the inhibitor by dividing the average value for wells containing compound by the average value for wells containing DMSO.(Only for Reference)
激酶實驗	FRET assay for HCV NS5A inhibitors: The peptide (Ac-Asp-Glu-Asp [EDANS]-Glu-Glu-Abu-[COO] Ala-Ser-Lys [DABCYL]-NH2) contains a fluorescence donor {EDANS, 5-[(2-aminoethyl)amino]naphthalene-1-sulfonic acid} near one end of the peptide and an acceptor {DABCYL, 4-[(4-dimethylamino)phenyl]azo)benzoic acid} near the other end. Intermolecular resonance energy transfer between the donor and the acceptor quenches the fluorescence of the peptide, but as the NS3 protease cleaves the peptide, the products are released from resonance energy transfer quenching. The fluorescence of the donor increases over time as more substrate is cleaved by the NS3 protease. The assay reagent is: 5× luciferase cell culture lysis reagent diluted to 1× with dWater, NaCl (150 mM), the FRET peptide (20 μM). HCV-Huh-7 cells are placed in a 96-well plate, and allowed to attach overnight (1×104 cells per well). The next day, BMS-790052 is added to the wells and the plate is incubated for 72 hours. The plate is then rinsed with PBS and used for the FRET assay by the addition of 30 μL of the FRET peptide assay reagent (described above) per well. Signals are obtained using the Cytofluor 4000 instrument, which has been set to 340 nm (excitation)/490 nm (emission) automatic mode, for 20 cycles or less, with the plate being read in the kinetic mode. Following FRET, 40 μL of luciferase substrate is added to each well and the luciferase is measured.
體外活性	Daclatasvir是迄今為止報道中的高效 HCV復制抑制劑。對于HCV基因型1a和1b復制子，Daclatasvir的平均EC50值分別為50和9pM。Daclatasvir顯示出至少105的治療指數(shù)(CC50/EC50)，并且對于一組10種RNA和DNA病毒無效，其EC50值高于10μM，這證實了Daclatasvir對HCV的特異性。[1]在含有HCV基因型1b復制子的Huh7細胞中，Daclatasvir能夠阻斷HCV基因組的瞬時和穩(wěn)定復制，EC50值范圍從1-15 pM不等。100 pM或1 nM的Daclatasvir已顯示出能改變NS5A的亞細胞定位和生化分級。[2]Daclatasvir抑制含有HCV基因型-4 NS5A基因的雜交復制子，EC50為7-13 pM。在雜交復制子中，NS5A的第30殘基是Daclatasvir介導的抗性的一個重要位點。[3]
體內(nèi)活性	在一項隨機、雙盲、安慰劑對照的單次遞增劑量研究中，Daclatasvir (BMS-790052) 以口服溶液形式，按六個劑量級別給予健康的非HCV感染受試者，劑量范圍從1到200mg。Daclatasvir在高達200mg的劑量下安全且耐受良好，無臨床相關(guān)不良反應。口服后，Daclatasvir迅速被吸收，暴露量與劑量成比例，且所有受試者在給藥后24小時及以后的化合物濃度均高于基于蛋白質(zhì)結(jié)合調(diào)整的EC90（針對基因型1a和1b，通過復制體測定法測量）[1]。小鼠分為兩組進行治療，一組接受Asunaprevir/Daclatasvir治療4周，另一組接受Ledipasvir/GS-558093治療4周。Asunaprevir/Daclatasvir和Ledipasvir/GS-558093治療能迅速降低血清HCV RNA水平至靈敏度以下，除Ledipasvir/GS-558093組的兩只小鼠外，治療完成后未檢測到病毒[5]。
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	H2O : < 1 mg/mL (insoluble or slightly soluble) DMSO : 136 mg/mL (184.1 mM) Ethanol : 136 mg/mL (184.1 mM)
關(guān)鍵字	antiviral \| Inhibitor \| genotypes \| EBP883 \| EBP-883 \| BMS790052 \| NS5A \| OATP1B1 \| Hepatitis C virus \| OATP1B3 \| HCV \| replicon \| BMS 790052 \| Daclatasvir \| inhibit \| JFH-1
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上市及藥典收錄分子庫 \| 高選擇性抑制劑庫 \| FDA 上市藥物庫 \| 抗病毒庫 \| 藥物功能重定位化合物庫 \| 人代謝物化合物庫

關(guān)鍵字：達拉他韋|||達卡他韋|||EBP 883|||Daklinza|||BMS-790052|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)和生物學研究的科學家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務。公司下設篩選事業(yè)部，化學事業(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；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)秀的供應商，為超過五百家學校和各類企業(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)	化學試劑,生物活性小分子	經(jīng)營模式	貿(mào)易,試劑,定制,服務

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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