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Daclatasvir

产品编号 T6229Cas号 1009119-64-5
别名 Daklinza, 达卡他韦, EBP 883, BMS-790052, 达拉他韦

Daclatasvir (EBP 883) 是一种高度选择性的 HCV NS5A 抑制剂,EC50 为 9-50 pM,适用于细胞培养中的多种 HCV 复制子基因型和 JFH-1 基因型 2a 感染性病毒。

Daclatasvir

Daclatasvir

纯度: 99.81%
产品编号 T6229 别名 Daklinza, 达卡他韦, EBP 883, BMS-790052, 达拉他韦Cas号 1009119-64-5

Daclatasvir (EBP 883) 是一种高度选择性的 HCV NS5A 抑制剂,EC50 为 9-50 pM,适用于细胞培养中的多种 HCV 复制子基因型和 JFH-1 基因型 2a 感染性病毒。

规格价格库存数量
1 mg¥ 223现货
5 mg¥ 497现货
10 mg¥ 756现货
25 mg¥ 1,560现货
50 mg¥ 3,110现货
100 mg¥ 4,560现货
200 mg¥ 6,490期货
1 mL x 10 mM (in DMSO)¥ 635现货
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纯度:99.81%
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产品介绍

生物活性
产品描述
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.
靶点活性
HCV NS5A:9 pM-50 pM(EC50)
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]。
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.
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)
别名Daklinza, 达卡他韦, EBP 883, BMS-790052, 达拉他韦
化学信息
分子量738.88
分子式C40H50N8O6
CAS No.1009119-64-5
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 136 mg/mL (184.1 mM)
Ethanol: 136 mg/mL (184.1 mM)
溶液配制表
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.3534 mL6.7670 mL13.5340 mL67.6700 mL
5 mM0.2707 mL1.3534 mL2.7068 mL13.5340 mL
10 mM0.1353 mL0.6767 mL1.3534 mL6.7670 mL
20 mM0.0677 mL0.3383 mL0.6767 mL3.3835 mL
50 mM0.0271 mL0.1353 mL0.2707 mL1.3534 mL
100 mM0.0135 mL0.0677 mL0.1353 mL0.6767 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

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent 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 μLDMSOTargetMol | reagent ( 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 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

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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