达拉他韦|T6229|TargetMol

Daclatasvir
1009119-64-5

￥223 1mg 起订

￥497 5mg 起订

￥756 10mg 起订

上海更新日期：2024-12-02

TargetMol中国（陶术生物）

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产品详情:

中文名称：: 达拉他韦

英文名称：: Daclatasvir

CAS号：: 1009119-64-5

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.

纯度规格：: 99.81%

产品类别：: 抑制剂

货号：: T6229

Product Introduction

Bioactivity

名称	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.
细胞实验	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)
激酶实验	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.
体外活性	Daclatasvir是迄今为止报道中的高效 HCV复制抑制剂。对于HCV基因型1a和1b复制子，Daclatasvir的平均EC50值分别为50和9pM。Daclatasvir显示出至少105的治疗指数(CC50/EC50)，并且对于一组10种RNA和DNA病毒无效，其EC50值高于10μM，这证实了Daclatasvir对HCV的特异性。[1]在含有HCV基因型1b复制子的Huh7细胞中，Daclatasvir能够阻断HCV基因组的瞬时和稳定复制，EC50值范围从1-15 pM不等。100 pM或1 nM的Daclatasvir已显示出能改变NS5A的亚细胞定位和生化分级。[2]Daclatasvir抑制含有HCV基因型-4 NS5A基因的杂交复制子，EC50为7-13 pM。在杂交复制子中，NS5A的第30残基是Daclatasvir介导的抗性的一个重要位点。[3]
体内活性	在一项随机、双盲、安慰剂对照的单次递增剂量研究中，Daclatasvir (BMS-790052) 以口服溶液形式，按六个剂量级别给予健康的非HCV感染受试者，剂量范围从1到200mg。Daclatasvir在高达200mg的剂量下安全且耐受良好，无临床相关不良反应。口服后，Daclatasvir迅速被吸收，暴露量与剂量成比例，且所有受试者在给药后24小时及以后的化合物浓度均高于基于蛋白质结合调整的EC90（针对基因型1a和1b，通过复制体测定法测量）[1]。小鼠分为两组进行治疗，一组接受Asunaprevir/Daclatasvir治疗4周，另一组接受Ledipasvir/GS-558093治疗4周。Asunaprevir/Daclatasvir和Ledipasvir/GS-558093治疗能迅速降低血清HCV RNA水平至灵敏度以下，除Ledipasvir/GS-558093组的两只小鼠外，治疗完成后未检测到病毒[5]。
存储条件	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)
关键字	antiviral \| Inhibitor \| genotypes \| EBP883 \| EBP-883 \| BMS790052 \| NS5A \| OATP1B1 \| Hepatitis C virus \| OATP1B3 \| HCV \| replicon \| BMS 790052 \| Daclatasvir \| inhibit \| JFH-1
相关产品	Resiquimod \| RO8191 \| Honokiol \| Grazoprevir \| Artemisinin \| EIDD-1931 \| Methyl 2-amino-5-bromobenzoate \| Deferiprone \| HCV-IN-30 \| Ribavirin \| HCV-IN-29 \| Sofosbuvir
相关库	抑制剂库 \| 经典已知活性库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA上市及药典收录分子库 \| 高选择性抑制剂库 \| FDA 上市药物库 \| 抗病毒库 \| 药物功能重定位化合物库 \| 人代谢物化合物库

达拉他韦|||达卡他韦|||EBP 883|||Daklinza|||BMS-790052|TargetMol

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	(12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