Daclatasvir (BMS-790052)
别名: EBP883 中文名称：达卡他韦
Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂，EC50为9-50 pM，在细胞培养中，作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。
Daclatasvir (BMS-790052) Chemical Structure
CAS: 1009119-64-5
客户使用Selleck的Daclatasvir (BMS-790052)发表文献52篇
产品质控
批次：
纯度：
99.70%
99.70
相关信号通路图
HCV Protease抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| GS4.3 | Antiviral assay | 0.15 uM | 6 days | Antiviral activity against HCV infected in human GS4.3 cells assessed as inhibition of NS3/4A levels at 0.15 uM treated with fresh media containing compound every 2 days measured after 6 days by Western blot method | 29232582 |
| GS4.3 | Antiviral assay | 0.15 uM | 6 days | Antiviral activity against HCV infected in human GS4.3 cells assessed as inhibition of viral core protein levels at 0.15 uM treated with fresh media containing compound every 2 days measured after 6 days by Western blot method | 29232582 |
| Huh7.5.1 | Antiviral assay | 100 pM to 1 uM | Antiviral activity against HCV genotype 1b NK/R2AN infected in human Huh7.5.1 cells expressing NS5A L31V mutant assessed as reduction in virus replication at 100 pM to 1 uM by luciferase reporter gene assay | 26134551 | |
| Huh7.5.1 | Antiviral assay | 100 pM to 1 uM | Antiviral activity against HCV genotype 1b NK/R2AN infected in human Huh7.5.1 cells expressing NS5A Y93H mutant assessed as reduction in virus replication at 100 pM to 1 uM by luciferase reporter gene assay | 26134551 | |
| Huh-luc/neo-ET replicon | Antiviral assay | 48 hrs | Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A L28V mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.000004μM | 24568313 | |
| Huh7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in human Huh7 cells after 3 days by cell-based replicon assay, EC50=0.000003μM | 25148100 | |
| human CEM cells | Cytotoxicity assay | 3 days | Cytotoxicity against human CEM cells after 3 days, CC50=9.6 μM | 25154714 | |
| HuH-Lcu-Neo | Function assay | 48 hrs | Inhibition of NS5A in HCV genotype 1b infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0000081μM | 32202782 | |
| Huh-5.2 | Antiviral assay | 4 days | Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-5.2 cells assessed as decrease in HCV replicon RNA replication after 4 days by luciferase assay, EC50=0.000009μM | 24900811 | |
| HuH7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay, EC50=0.000009μM | 24320933 | |
| HuH7 | Antiviral assay | 72 hrs | Antiviral activity against HCV1b infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC50=0.000009μM | 24521299 | |
| Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo | Function assay | 72 hrs | Inhibition of NS5A in HCV genotype 2a infected in human Huh7.5/J6/JFH1/EMCVIRES/hRlucNeo cells assessed as inhibition of replicon levels incubated for 72 hrs by luciferase reporter gene assay, IC50=0.000009μM | 31710479 | |
| HuH7 replicon | Function assay | 2 days | Inhibition of NS5A in HCV genotype 1b infected in human HuH7 replicon cells assessed as reduction in subgenomic viral RNA replication treated for 2 days followed by compound washout and subsequent compound dosing measured after 1 day by SEAP reporter gene, EC50=0.000009μM | 30772607 | |
| Huh-luc/neo-ET replicon | Antiviral assay | 48 hrs | Antiviral activity against Hepatitis C virus genotype 1b in Huh-luc/neo-ET replicon cells after 48 hrs by replicon-based luciferase assay, EC50=0.00001μM | 24568313 | |
| HuH7.5/Con1/SG-Neo(I)-hRluc2aUb | Function assay | 72 hrs | Inhibition of NS5A in HCV genotype 1b infected in human HuH7.5/Con1/SG-Neo(I)-hRluc2aUb cells assessed as inhibition of replicon levels incubated for 72 hrs by luciferase reporter gene assay, IC50=0.000023μM | 31710479 | |
| HuH-Lcu-Neo | Function assay | 48 hrs | Inhibition of NS5A in HCV genotype 1a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0000324μM | 32202782 | |
| Huh-luc/neo-ET replicon | Antiviral assay | 48 hrs | Antiviral activity against Hepatitis C virus genotype 1a in Huh-luc/neo-ET replicon cells after 48 hrs by replicon-based luciferase assay, EC50=0.0000398μM | 24568313 | |
| W11.8 | Antiviral assay | 4 days | Antiviral activity against Hepatitis C virus genotype 1a infected in W11.8 cells assessed as decrease in NS5A expression in replicon cell after 4 days by luminescence based ELISA, EC50=0.00005μM | 24900811 | |
| HuH7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1a H77 infected in human HuH7 cells assessed as inhibition of viral RNA replication after 3 days by renilla luciferase reporter gene assay, EC50=0.00005μM | 24320933 | |
| HuH7 | Antiviral assay | 72 hrs | Antiviral activity against HCV1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC50=0.00005μM | 24521299 | |
| HuH-Lcu-Neo | Function assay | 48 hrs | Inhibition of NS5A in patient-derived HCV genotype 3a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0001145μM | 32202782 | |
| Huh-luc/neo-ET replicon | Antiviral assay | 48 hrs | Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A L31V mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.0001259μM | 24568313 | |
| Huh-luc/neo-ET replicon | Antiviral assay | 48 hrs | Antiviral activity against Hepatitis C virus genotype 1b harboring NS5A Y93H mutant gene in Huh-luc/neo-ET replicon cells after 48 hrs by transient replicon mutant-based luciferase assay, EC50=0.0003162μM | 24568313 | |
| HuH7 | Antiviral assay | 72 hrs | Antiviral activity against HCV1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by FRET assay, EC90=0.00038μM | 24521299 | |
| HuH-Lcu-Neo | Function assay | 48 hrs | Inhibition of NS5A in HCV genotype 3a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0004115μM | 32202782 | |
| HuH-Lcu-Neo | Function assay | 48 hrs | Inhibition of NS5A in patient-derived HCV genotype 2a infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.0494μM | 32202782 | |
| HuH-Lcu-Neo | Function assay | 48 hrs | Inhibition of NS5A in HCV genotype 2a con infected in HuH-Lcu-Neo cells assessed as reduction in viral replication incubated for 48 hrs by luciferase reporter gene assay, EC50=0.05285μM | 32202782 | |
| CEM | Cytotoxicity assay | 3 days | Cytotoxicity against human CEM cells after 3 days, CC50=9.6μM | 22507961 | |
| Vero | Cytotoxicity assay | 3 days | Cytotoxicity against african green monkey Vero cells after 3 days, CC50=21μM | 22507961 | |
| HuH7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in human HuH7 cells at >= 10 times antiviral EC50 after 3 days by luciferase reporter assay | 28430437 | |
| HuH7 | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in human HuH7 cells co-treated with asunaprevir after 3 days by luciferase reporter assay | 28430437 | |
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000004μM | 26099532 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV1b infected in human HuH7 cells assessed as inhibition of viral replication by RT-PCR analysis, EC50=0.0000066μM | 22507961 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1b Con1 infected in human HuH7 cells assessed as inhibition of viral replication, EC50=0.000009μM | 26077493 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV 1b infected in human HuH7 cells by in vitro replicon assay, EC50=0.00001μM | 23466233 | ||
| HuH7 | Function assay | Inhibition of NS5A in HCV genotype-1b infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000023μM | 25453810 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1b JFH-1 infected in human HuH7 cells assessed as inhibition of viral replication, EC50=0.000028μM | 26077493 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV 1b infected in human HuH7 cells by in vitro replicon assay, EC90=0.00003μM | 23466233 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1b expressing NS5A L31V mutant infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000035μM | 26099532 | ||
| HuH7 | Antiviral assay | Antiviral activity against wild type HCV genotype 1b infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.000048μM | 26099532 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 5a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000051μM | 25453811 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1b infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.000073μM | 25453811 | ||
| HuH7 | Function assay | Inhibition of NS5A in HCV genotype-1a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00014μM | 25453810 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00014μM | 25453811 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 1b expressing NS5A Y93H mutant infected in human HuH7 cells assessed as reduction in viral RNA replication, EC50=0.00018μM | 26099532 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 4a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00041μM | 25453811 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 6a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00045μM | 25453811 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 3a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00067μM | 25453811 | ||
| HuH7 | Antiviral assay | Antiviral activity against HCV genotype 2a infected in human HuH7 cells by luciferase reporter gene assay, EC50=0.00067μM | 25453811 | ||
| CEM | Cytotoxicity assay | Cytotoxicity against human CEM cells, CC50=9.6μM | 22704887 | ||
| Vero | Cytotoxicity assay | Cytotoxicity against african green monkey Vero cells, CC50=9.6μM | 23466233 | ||
| CEM | Cytotoxicity assay | Cytotoxicity against human CEM cells, CC50=10μM | 26099532 | ||
| PBMC | Cytotoxicity assay | Cytotoxicity against human PBMC cells, CC50=19μM | 22704887 | ||
| Vero | Cytotoxicity assay | Cytotoxicity against african green monkey Vero cells, CC50=21μM | 22704887 | ||
| CEM | Cytotoxicity assay | Cytotoxicity against human CEM cells, CC50=21μM | 23466233 | ||
| Vero | Cytotoxicity assay | Cytotoxicity against african green monkey Vero cells, CC50=21μM | 26099532 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Daclatasvir (BMS-790052, EBP883) 是一种高度选择性的HCV NS5A抑制剂，EC50为9-50 pM，在细胞培养中，作用于多种HCV复制基因型和JFH-1基因型2a的感染性病毒。Phase 3。 | ||
|---|---|---|---|
| 特性 | BMS-790052是一流的高选择性C型肝炎病毒(HCV) NS5A抑制剂， EC50为皮摩尔级。 | ||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | BMS-790052是到目前为止报道的最有效的HCV复制抑制剂之一,作用于HCV基因型1a和1b复制子时EC50分别为50和9 pM。 BMS-790052治疗指数(CC50/EC50)为105以上，对一组10种RNA和DNA病毒没有作用效果, EC50大于10 μM, BMS-790052只针对HCV有效。[1] BMS-790052作用于含HCV基因型1b复制子的Huh7细胞, BMS-790052抑制短暂和稳定的HCV染色体复制, EC50为1-15 pM。BMS-790052 (100 pM或1 nM)改变NS5A的亚细胞定位和生化结构。[2] BMS-790052抑制含HCV基因型-4 NS5A基因的杂合复制子，EC50为7-13 pM。杂合复制子中的NS5A残基30是BMS-790052选择耐抗性的一个重要位点。[3] | |||
|---|---|---|---|---|
| 激酶实验 | 针对HCV NS5A抑制剂的FRET实验 | |||
| 肽段 (Ac-Asp-Glu-Asp [EDANS]-Glu-Glu-Abu-[COO] Ala-Ser-Lys [DABCYL]-NH2)含荧光供体{EDANS, 5-[(2-氨乙基)氨基]萘-1-磺酸} ，位于肽段一端；受体 {DABCYL, 4-[4-(二甲基氨基)苯偶氮]苯甲酸}，位于肽段另一端。通过在供体和受体之间分子能量共振转移使肽段荧光淬灭，NS3蛋白酶使肽段断裂，共振能量转移淬灭使产物释放，供体的荧光随着底物被NS3蛋白酶降解的时间而增强。反应所用试剂如下：5×荧光素酶细胞培养液用dH2O稀释到1×,NaCl (150 mM), FRET肽(20 μM)。HCV-Huh-7细胞按每孔1×104个接种在96孔板上，粘附过夜。 第二天, BMS-790052加到孔中，温育72小时。用PBS冲洗板，每孔加入30 μL FRET肽实验试剂进行FRET实验。使用Cytofluor 4000仪测定吸光值。随后，40 μL荧光素酶底物加到每孔中，测定荧光值。 | ||||
| 细胞实验 | 细胞系 | HCV复制子细胞(Huh7) | ||
| 浓度 | 0.1 pM-50 µM, 溶于DMSO，最终DMSO浓度为0.5% | |||
| 孵育时间 | 72小时 | |||
| 方法 | 细胞接种在96孔板上的200µL培养基中，12小时后，BMS-790052加到含HCV复制子的96孔板上。温育72小时，测定复制活性和细胞毒性。使用CellTiter-Blue测定细胞毒性。随后，移除培养基和染料，使板倒转，残留的液体用纸巾吸干，使用Renilla荧光素酶测定HCV 基因型1a细胞系的复制活性。1×Renilla荧光素酶溶解buffer (30 µL)加到每孔中，温和震荡15分钟。加入Renilla荧光素酶底物(40 µL)， 使用Top Count光度计测定信号。 | |||
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT05992077 | Not yet recruiting | HCV Infection |
ANRS Emerging Infectious Diseases |
August 7 2023 | Not Applicable |
| NCT04852614 | Recruiting | Hepatitis C Virus Infection |
Ain Shams University |
December 1 2020 | -- |
| NCT04773756 | Completed | Covid19 |
Alexandria University |
November 1 2020 | Phase 4 |
| NCT03208322 | Withdrawn | Hepatitis C |
Bristol-Myers Squibb |
November 30 2018 | -- |
化学信息&溶解度
| 分子量 | 738.88 | 分子式 | C40H50N8O6 |
| CAS号 | 1009119-64-5 | SDF | Download Daclatasvir (BMS-790052) SDF |
| Smiles | CC(C)C(C(=O)N1CCCC1C2=NC=C(N2)C3=CC=C(C=C3)C4=CC=C(C=C4)C5=CN=C(N5)C6CCCN6C(=O)C(C(C)C)NC(=O)OC)NC(=O)OC | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 148 mg/mL ( (200.3 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 148 mg/mL Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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