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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Boceprevir
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
394730-60-0
- 规格：
100mg/50mg/25mg/10mg/5mg
| 规格： | 100mg | 产品价格： | ￥3365.0 |
|---|---|---|---|
| 规格： | 50mg | 产品价格： | ￥2240.0 |
| 规格： | 25mg | 产品价格： | ￥1581.0 |
| 规格： | 10mg | 产品价格： | ￥890.0 |
| 规格： | 5mg | 产品价格： | ￥588.0 |
| 基本信息 | |
| CAS | No.394730-60-0 |
| 中文名称 | 波普瑞韦 |
| 英文名称 | Boceprevir |
| 别名 | SCH 503034;EBP 520 |
| 分子式 | C27H45N5O5 |
| 分子量 | 519.68 |
| 溶解性 | Soluble in DMSO |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:-20℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| EC | EINECS 800-043-2 |
| MDL | MFCD22208555 |
| SMILES | O=C(N1[C@@H]([C@@]2([H])C(C)([C@]2(C1)[H])C)C(NC(C(C(N)=O)=O)CC3CCC3)=O)[C@@H](NC(NC(C)(C)C)=O)C(C)(C)C |
| 靶点 | HCV Protease |
| 通路 | Metabolic Enzyme/Protease |
| 背景说明 | Boceprevir是一种有效的选择性的 HCV NS3 protease 抑制剂。 |
| 生物活性 | Boceprevir is a potent， highly selective， orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay[1][2][3][4][5]. Boceprevir inhibits SARS-CoV-2 3CLpro activity[6]. |
| IC50 | Ki: 14 nM (HCV NS3 protease)[1] |
| In Vitro | Boceprevir is a potent inhibitor in both Enzyme assay (Ki* = 14 nM) and cell-based replicon assay (EC 90 = 0.35 microM). It is highly selective (2200x) against human neutrophil Elastase (HNE). [1]。 |
| 细胞实验 | In the current study， we generated a novel NS3/4A/Lap/LC - 1 triple - transgenic mouse model that can be used to evaluate and screen NS3/4A Protease Inhibitors.The NS3/4A protease could be conditionally inducibly expressed in the livers of the triple - transgenic mice using a dual Tet - On and Cre/loxP system. In this system， doxycycline (Dox) induction resulted in the secretion of Gaussia luciferase (Gluc) into the blood， and this secretion was dependent on NS3/4A protease - mediated cleavage at the 4B5A junction. Accordingly， NS3/4A protease activity could be quickly assessed in real time simply by monitoring Gluc activity in plasma. The results from such monitoring showed a 70 - fold increase in Gluc activity levels in plasma samples collected from the triple - transgenic mice after Dox induction. Additionally， this enhanced plasma Gluc activity was well correlated with the induction of NS3/4A protease expression in the liver.Following oral administration of the commercial NS3/4A - specific inhibitors telaprevir and boceprevir， plasma Gluc activity was reduced by 50% and 65%， respectively.[2] |
| 动物实验 | Mice[2]:Boceprevir is purchased from MedChem Express. To evaluate the effect of Boceprevir， triple-transgenic mice are induced with Doxycycline (Dox) for 10 days (n=5 per group). On the third day after Dox induction， when plasma Gluc activity reaches its peak， the mice are administered either Boceprevir (100 mg/kg) or DMSO via oral gavage twice daily for 7 days. During this period， blood is collected from the caudal vein daily to detect plasma Gluc activity. |
| 数据来源文献 | [1]. Njoroge FG， et al. Challenges in modern drug discovery: a case study of boceprevir， an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41(1):50-9. [2]. Yao M， et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11(3):e0150894. [3]. Coilly A， et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56(11):5728-34. [4]. Berenguer M， et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56. [5]. Burton MJ， et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105(8):431-6. [6]. Qi Sun， et al. Bardoxolone and bardoxolone methyl， two Nrf2 activators in clinical trials， inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. |
| 单位 | 瓶 |
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IB1770 波普瑞韦 抗感染 索莱宝
￥588 - 3365
