化学信息：
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化学名
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(1R,2S)-N-[[[(1R,2R)-2-[5-(3-Hydroxy-6-methoxy-2-quinoxalinyl)pentyl]cyclopropyl]oxy]carbonyl]-3-methyl-L-valyl-(4R)-4-hydroxy-L-prolyl-1-amino-N-(cyclopropylsulfonyl)-2-ethenylcyclopropanecarboxamide cyclic (1→;2)-ether
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简称
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MK5172
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别名
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Grazoprevir, MK 5172, MK5172
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中文名
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N/A
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化学式
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C38H50N6O9S
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分子量
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766.9
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CAS号
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1350514-68-9
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO10mg/ml; Ethanol<1mg/ml
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溶液配制
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5mg加入0.65ml DMSO，或者每7.67mg加入1ml DMSO，配制成10mM溶液。SC3260-10mM用DMSO配制。
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生物信息：
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产品描述
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MK-5172 is a novel P2-P4 quinoxaline macrocyclic HCV NS3/4a protease inhibitor currently in clinical development.
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信号通路
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Anti-infection; Metabolism; Proteases
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靶点
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genotype 1b
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genotype 1a
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－
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－
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－
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IC50
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7.4nM
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7nM
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－
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－
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－
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体外研究
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In biochemical assays, MK-5172 was effective against a panel of major genotypes and variants engineered with common resistant mutations observed in clinical studies with other NS3/4a protease inhibitors. In the replicon assay, MK-5172 demonstrated subnanomolar to low-nanomolar EC50s against genotypes 1a, 1b, and 2a.
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体内研究
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In rats, MK-5172 showed a plasma clearance of 28ml/min/kg and plasma half-life of 1.4hr. When dosed p.o. at 5mg/kg, the plasma exposure of MK-5172 was good with an AUC of 0.7μM.hr. The liver exposure of the compound was quite good (23μM at 4hr), and MK-5172 remained in liver 24hr after a single p.o. 5mg/kg dose. At 24hr, the liver concentration of MK-5172 was 0.2μM, which was over 25-fold higher than the IC50 in the replicon assay with 50% NHS. When dosed to dogs, MK-5172 showed low clearance of 5ml/min/kg and a 3hr half-life after i.v. 2mg/kg dosing and had good plasma exposure (AUC=0.4μM.hr) after a p.o. 1mg/kg dose.
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临床实验
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Evaluation of Hepatic Pharmacokinetics for MK-5172 in Participants With Chronic Hepatitis C. Phase 1.
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特征
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N/A
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相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Steven Harper, John A. McCauley, Michael T. ACS Med. Chem. Lett. 2012, 3(4), 332-336.
2. Summa V, Ludmerer SW, McCauley JA. Antimicrob Agents Chemother. 2012 Aug, 56(8), 4161-7.
包装清单：
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产品编号
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产品名称
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包装
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SC3260-10mM
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MK5172 (HCV抑制剂)
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10mM×0.2ml
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SC3260-5mg
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MK5172 (HCV抑制剂)
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5mg
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SC3260-25mg
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MK5172 (HCV抑制剂)
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25mg
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—
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说明书
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1份
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保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
注意事项：
本产品对人体有害，操作时请小心，并注意有效防护以避免直接接触人体或吸入体内。
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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