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Asunaprevir
別名: BMS-650032 中文名稱：阿那匹韋
Asunaprevir是具有口服活性的HCV NS3抑制劑。HCV NS3是病毒復制蛋白加工所必需的蛋白酶。
Asunaprevir Chemical Structure
CAS: 630420-16-5
產(chǎn)品質(zhì)控
批次：
純度：
99.99%
99.99
Asunaprevir相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | Lomibuvir (VX-222) Danoprevir PSI-6206 (GS-331007) | 點擊展開 |
|---|---|---|
| 相關(guān)化合物庫 | FDA藥物庫 天然產(chǎn)物庫 已知活性藥物庫-I 蛋白酶抑制劑庫 泛素化化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| Huh7.5 replicon cells | Antiviral assay | 4 days | Antiviral activity against HCV genotype 1b infected in human Huh7.5 replicon cells assessed as reduction in viral replication incubated for 4 days by luciferase reporter gene assay, EC50=0.006μM | 29650290 | |
| HuH7.5 cells | Antiviral assay | 4 days | Antiviral activity against HCV genotype 1b Con1 infected in human HuH7.5 cells assessed as inhibition of viral replication after 4 days by luciferase reporter gene assay, EC50=0.006μM | 29456803 | |
| HuH7 replicon cells | Function assay | 4 days | Inhibition of HCV genotype 1a H77 NS3 protease infected in human HuH7 replicon cells assessed as reduction in viral replication after 4 days by luciferase reporter gene assay, EC50=0.004μM | 29162454 | |
| HuH7 replicon cells | Function assay | 4 days | Inhibition of HCV genotype 1b Con1 NS3 protease infected in human HuH7 replicon cells assessed as reduction in viral replication after 4 days by luciferase reporter gene assay, EC50=0.0012μM | 29162454 | |
| HuH7 cells | Antiviral assay | 3 days | Antiviral activity against HCV genotype 1b infected in human HuH7 cells co-treated with daclatasvir after 3 days by luciferase reporter assay | 28430437 | |
| HuH7 cells | 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 | |
| genotype 2a replicon cells | Function assay | Inhibition of recombinant full length HCV genotype 3a S52 NS3 protease in genotype 2a replicon cells by luciferase reporter gene assay, EC50=1.1μM | 27564532 | ||
| genotype 2a replicon cells | Function assay | Inhibition of recombinant full length HCV genotype 2b HC-J8 NS3 protease in genotype 2a replicon cells by luciferase reporter gene assay, EC50=0.621μM | 27564532 | ||
| HCV replicon cells | Antiviral assay | Antiviral activity against HCV genotype 2a JHF-1 in HCV replicon cells assessed as reduction in viral RNA replication by luciferase reporter gene assay, EC50=0.217μM | 27564532 | ||
| HCV replicon cells | Antiviral assay | Antiviral activity against HCV genotype 1a H77 in HCV replicon cells assessed as reduction in viral RNA replication by luciferase reporter gene assay, EC50=0.004μM | 27564532 | ||
| Huh7.5 cells | Antiviral assay | Antiviral activity against HCV genotype 1b Con1 expressing NS3 protease infected in human Huh7.5 cells assessed as reduction in viral RNA replication by luciferase reporter gene assay, EC50=0.003μM | 27564532 | ||
| genotype 1b con1 replicon cells | Function assay | Inhibition of recombinant full length HCV genotype 4a ED43 NS3 protease in genotype 1b con1 replicon cells by luciferase reporter gene assay, EC50=0.0017μM | 27564532 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Asunaprevir是具有口服活性的HCV NS3抑制劑。HCV NS3是病毒復制蛋白加工所必需的蛋白酶。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點 |
|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03208322 | Withdrawn | Hepatitis C |
Bristol-Myers Squibb |
November 30 2018 | -- |
| NCT03004625 | Completed | Hepatitis C |
Kaohsiung Medical University Chung-Ho Memorial Hospital|Chang Gung Memorial Hospital|National Taiwan University Hospital|Taipei Veterans General Hospital Taiwan|China Medical University Hospital|National Cheng-Kung University Hospital |
November 2016 | Phase 3 |
| NCT02865369 | Unknown status | Chronic Hepatitis C |
Sang Gyune Kim|Seoul National University Boramae Hospital|Severance Hospital|Inha University Hospital|Korea University|Gachon University Gil Medical Center|Hanyang University Seoul Hospital|Ewha Womans University Mokdong Hospital|Bristol-Myers Squibb|Soonchunhyang University Hospital |
September 2016 | -- |
| NCT02580474 | Completed | Hepatitis C |
Myeong Jun Song|Bristol-Myers Squibb|Soonchunhyang University Hospital|Dankook University|Chungnam National University Hospital|Konyang University Hospital|Eulji University Hospital|Saint Vincent''s Hospital Korea|Konkuk University Hospital|Cheongju St. Mary''s Hospital Cheongju Korea|Severance Hospital|Korea University Guro Hospital|Eulji General Hospital|The Catholic University of Korea |
February 2016 | Phase 4 |
| NCT02496078 | Completed | Hepatitis C |
Bristol-Myers Squibb |
August 2015 | Phase 3 |
| NCT02309450 | Withdrawn | Hepatitis C Virus Genotype 4 Infection |
ANRS Emerging Infectious Diseases|Bristol-Myers Squibb |
December 2014 | Phase 2 |
化學信息&溶解度
| 分子量 | 748.29 | 分子式 | C35H46ClN5O9S |
| CAS號 | 630420-16-5 | SDF | -- |
| Smiles | CC(C)(C)C(C(=O)N1CC(CC1C(=O)NC2(CC2C=C)C(=O)NS(=O)(=O)C3CC3)OC4=NC=C(C5=C4C=C(C=C5)Cl)OC)NC(=O)OC(C)(C)C | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (133.63 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 100 mg/mL (133.63 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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