Grazoprevir
别名: MK5172 中文名称：格佐匹韦，格拉瑞韦
Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂，HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。
Grazoprevir Chemical Structure
CAS: 1350514-68-9
客户使用Selleck的发表文献6篇
产品质控
Grazoprevir相关产品
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 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Grazoprevir anhydrous (MK5172) 是一种 Hepatitis C Virus NS3/4A Protease 的抑制剂，HCV genotype 1a、1B和4的IC50值分别为7pM、4pM和62pM。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
|
| 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 |
化学信息&溶解度
| 分子量 | 766.9 | 分子式 | C38H50N6O9S |
| CAS号 | 1350514-68-9 | SDF | Download Grazoprevir SDF |
| 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 | ||
| 储存条件(自收到货起) | |||
|
体外溶解度 |
DMSO : 100 mg/mL ( (130.39 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 100 mg/mL Water : Insoluble |
摩尔浓度计算器 |
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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）
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）
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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