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

Grazoprevir

別名：MK5172

Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively.

Grazoprevir化学構造

CAS No. 1350514-68-9

サイズ 価格(税別) 在庫状況
JPY 23500 国内在庫あり
JPY 44500 国内在庫あり
JPY 145500 国内在庫あり
JPY 295500 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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製品安全説明書

現在のバッチを見る： 純度： 99.99%
99.99

Grazoprevir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 Antiviral assay 72 hrs Antiviral activity against HCV genotype 1a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR method, EC50=0.0003μM. 26819676
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR method, EC50=0.0003μM. 26819676
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 1a infected in human HuH7 cells assessed as reduction viral RNA level after 72 hrs by RT-PCR method, EC50=0.0006μM. 27994759
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 1b infected in human HuH7 cells assessed as reduction viral RNA level after 72 hrs by RT-PCR method, EC50=0.0006μM. 27994759
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 2a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR method, EC50=0.0012μM. 26819676
HuH7 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus genotype 1b infected in HuH7 cells assessed as reduction in replicon RNA level after 72 hrs by TaqMan-based RT-PCR analysis in presence of 10% FBS, EC50=0.0015μM. 24900818
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 2b infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR method, EC50=0.005μM. 26819676
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 2a infected in human HuH7 cells assessed as reduction viral RNA level after 72 hrs by RT-PCR method, EC50=0.0054μM. 27994759
HuH7 Antiviral assay 24 hrs Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs presence of 40% NHS, IC50=0.007μM. 24900473
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 3a infected in human HuH7 cells assessed as inhibition of viral replication after 72 hrs by RT-PCR method, EC50=0.0072μM. 26819676
HuH7 Antiviral assay 72 hrs Antiviral activity against HCV genotype 3a infected in human HuH7 cells assessed as reduction viral RNA level after 72 hrs by RT-PCR method, EC50=0.0072μM. 27994759
HuH7 Antiviral assay 24 hrs Antiviral activity against Hepatitis C virus (isolate Con1) genotype 1b infected in human HuH7 cells assessed as inhibition of viral replication after 24 hrs in presence of 50% NHS, IC50=0.0074μM. 24900473
HuH7 Antiviral assay 72 hrs Antiviral activity against Hepatitis C virus genotype 3a infected in HuH7 cells assessed as reduction in replicon RNA level after 72 hrs by TaqMan-based RT-PCR analysis in presence of 10% FBS, EC50=0.013μM. 24900818
HBI10A Antiviral assay Antiviral activity against Hepatitis C virus subtype 1b infected in HBI10A cells harboring HCV subgenomic bicistronic replicon assessed as reduction in viral replication, EC50=0.002μM. ChEMBL
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生物活性

製品説明 Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively.
Targets
gt1b [1]
(Cell-free assay)		 gt1a [1]
(Cell-free assay)		 gt1b R155K [1]
(Cell-free assay)		 gt2a [1]
(Cell-free assay)		 gt1b D168V [1]
(Cell-free assay)		 もっとクリックする
0.01 nM(Ki) 0.01 nM(Ki) 0.07 nM(Ki) 0.08 nM(Ki) 0.14 nM(Ki)
In Vitro
In vitro MK-5172 is a novel P2-P4 quinoxaline macrocyclic NS3/4a protease inhibitor currently in clinical development. The compound demonstrates subnanomolar activity against a broad enzyme panel encompassing major hepatitis C virus (HCV) genotypes as well as variants resistant to earlier protease inhibitors[1].
細胞実験 細胞株 HB1 cells
濃度 2, 5, or 10 nM
反応時間 1, 2, 3.5 days
実験の流れ 30,000 HB1 cells are seeded per well of a 6-well tissue culture plate per drug concentration. The next day (day 0), the medium is replenished with fresh medium and MK-5172 at the appropriate drug concentration. Cells from a single well per drug concentration are harvested on days 0, 1, and 2, washed, and stored frozen until evaluation. The fourth well is similarly harvested on day 3.5 except that 30,000 cells are reseeded with fresh medium and MK-5172 at the appropriate drug concentration. For additional time points, cells are passaged and harvested every one-half week for 2 weeks. For the third week, cells are similarly treated except that cells received replenishing medium which contained 0.5 mg/ml G418 without protease inhibitor.
In Vivo
In Vivo In both rat and dog, MK-5172 demonstrates good plasma and liver exposures, with 24-h liver levels suggestive of once-daily dosing. When administered to HCV-infected chimpanzees harboring chronic gt1a or gt1b infections, MK-5172 suppresses viral load between 4 to 5 logs at a dose of 1 mg/kg of body weight twice daily (b.i.d.) for 7 days. MK-5172 demonstrates low to moderate clearance and a modest half-life in both rat and dog. Upon oral administration, MK-5172 demonstrates modest bioavailability of 12 to 13%, with moderate plasma exposure in both species. Significant liver concentrations are achieved in both rat and dog. The 24-h trough liver concentrations are 0.2 μM in rat and 1.4 μM in dog (1 mg per kg), yielding exposure multiples of 27- to 200-fold over the serum-adjusted replicon EC50. MK-5172 proves highly efficacious in vivo at moderate doses against chronic-HCV-infected chimpanzees, including greater viral load suppression than vaniprevir when dosed alternatively to the same animal at an otherwise identical dose and frequency[1].
動物実験 動物モデル rats or dogs
投与量 2 mg/kg of body weight (rat) or 0.5 mg/kg (dog)
投与経路 i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03105349 Withdrawn
HCV
Fundacion SEIMC-GESIDA
 July 1 2017 Phase 4
NCT03145623 Completed
Hepatitis C|Chronic Kidney Diseases
University Hospital Toulouse|MSD France
 June 2 2017 --
NCT02973503 Completed
Chronic HCV Infection
University Hospital Clermont-Ferrand|Merck Sharp & Dohme LLC
 January 11 2017 Phase 3

化学情報

分子量 766.9 化学式

C38H50N6O9S
CAS No. 1350514-68-9 SDF Download Grazoprevir SDFをダウンロードする
Smiles CC(C)(C)C1C(=O)N2CC(CC2C(=O)NC3(CC3C=C)C(=O)NS(=O)(=O)C4CC4)OC5=NC6=C(C=CC(=C6)OC)N=C5CCCCCC7CC7OC(=O)N1
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (130.39 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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