ホームページ Proteases HCV Protease inhibitor Asunaprevir For research use only.

Asunaprevir

別名：BMS-650032

Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.

Asunaprevir化学構造

CAS No. 630420-16-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 44500 国内在庫あり
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
JPY 98500 国内在庫あり
JPY 235500 国内在庫なし(納期7~10日)
JPY 748500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Asunaprevir関連製品

シグナル伝達経路

HCV Protease Signaling Pathways

HCV Proteaseシグナル伝達経路

HCV Protease阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
Targets
1b (J4L6S) [1] 1a (H77) [1] 6a (HK-6A) [1] 4a (ED43) [1] 5a (SA13) [1] もっとクリックする
0.3 nM 0.7 nM 0.9 nM 1.6 nM 1.7 nM
In Vitro
In vitro Asunaprevir (ASV) competitively binds to the NS3/4A protease complex, with Ki values of 0.4 and 0.24 nM against recombinant enzymes representing genotypes 1a (H77) and 1b (J4L6S), respectively. Asunaprevir is high selective without any significant activity against the closely related GB virus-B NS3 protease and a panel of human serine or cysteine proteases. In cell culture, ASV inhibits replication of HCV replicons representing genotypes 1 and 4, with 50% effective concentrations (EC50s) ranging from 1 to 4 nM, and has weaker activity against genotypes 2 and 3 (EC50, 67-1162 nM). Selectivity is again demonstrated by the absence of activity (EC50, >12 μM) against a panel of other RNA viruses[1].
細胞実験 細胞株 Huh 7.5.1 cells
濃度 1 or 10 nM
反応時間 3, 6, 24, and 48 h
実験の流れ

--
In Vivo
In Vivo Plasma and tissue exposures in vivo in several animal species indicate that ASV displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species). Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50s observed with HCV genotype-1 replicons[1].
動物実験 動物モデル male FVB mice, Sprague-Dawley rats, male beagles, male cynomolgus monkeys
投与量 5 mg/kg (mice); 3, 5, 10, and 15 mg/kg (rats); 3 or 6 mg/kg (Dogs); 3 mg/kg (Monkeys)
投与経路 by oral gavage
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

化学情報

分子量 748.29 化学式

C35H46ClN5O9S
CAS No. 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
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (133.63 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 100 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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