Nesbuvir
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Nesbuvir是一种新型的选择性非结构蛋白5B(NS5B)聚合酶抑制剂,其 IC50值为5 nM [1]。
NS5B(非结构蛋白5B)是HCV中的病毒蛋白,在HCV RNA复制中,通过使用病毒正RNA链作为模板和催化rNTP的聚合发挥重要作用。作为HCV复制中主要的催化酶,NS5B是HCV-RNA复制可用的靶标,可以用于治疗HCV [2][3]。
Nesbuvir是选择性的NS5B聚合酶抑制剂,与已报道的ALK抑制剂crizotinib具有不同的选择性。使用Huh7.5细胞系进行测试,nesbuvir对NS5B和降低细胞敏感性的突变具有较高选择性 [1]。在Huh-7细胞衍生的克隆A细胞中,每个细胞含有约1000个基因组拷贝的HCV基因型1b复制子,用0.1 μM和1 μM的nesbuvir处理16天,HCV RNA水平减少约3.6 log10和4.2 log10 [2]。
在嵌合体小鼠模型中,nesbuvir导致HCV滴度减少2.02 +/- 0.55 log,当与干扰素联合使用,30 mg/kg剂量nesbuvir每日三次,具有2.44 log的减少,比单独使用干扰素有更好的治疗效果[4]。
参考文献:?
[1].?Flint, M., et al., Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). Antimicrob Agents Chemother, 2009. 53(2): p. 401-11.
[2].?Howe, A.Y., et al., Molecular mechanism of hepatitis C virus replicon variants with reduced susceptibility to a benzofuran inhibitor, HCV-796. Antimicrob Agents Chemother, 2008. 52(9): p. 3327-38.
[3].?Meshram, R.J. and R.N. Gacche, Effective epitope identification employing phylogenetic, mutational variability, sequence entropy, and correlated mutation analysis targeting NS5B protein of hepatitis C virus: from bioinformatics to therapeutics. J Mol Recognit, 2015.
[4]. Kneteman, N.M., et al., HCV796: A selective nonstructural protein 5B polymerase inhibitor with potent anti-hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus. Hepatology, 2009. 49(3): p. 745-52.
- 1. Yoshimi Shimizu, Takeru Suzuki, et al. "Antiviral Effects of the Anti-Occludin Monoclonal Antibody on Persistent Hepatitis C Virus Infection in a Human Liver Chimeric Mouse Model." BPB Reports 4,142-147(2021).
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 446.49 |
Cas No. | 691852-58-1 |
Formula | C22H23FN2O5S |
Synonyms | HCV 796;HCV-796;HCV796,Nesbuvir |
Solubility | ≥22.3 mg/mL in DMSO; insoluble in H2O; ≥97.8 mg/mL in EtOH with gentle warming |
Chemical Name | 5-cyclopropyl-2-(4-fluorophenyl)-6-[2-hydroxyethyl(methylsulfonyl)amino]-N-methyl-1-benzofuran-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | CNC(=O)C1=C(OC2=CC(=C(C=C21)C3CC3)N(CCO)S(=O)(=O)C)C4=CC=C(C=C4)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
Huh7-BB7细胞 |
溶解方法 |
在DMSO中的溶解度大于22.3 mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
7 d,40-80 nM |
应用 |
Nesbuvir是丙型肝炎病毒非结构蛋白5B(NS5B)聚合酶的抑制剂,它可以强效特异性地抑制HCV RNA 依赖性RNA 聚合酶,从而抑制RNA的合成。在负载亚基因组基因型1b HCV复制子的Huh7-BB7细胞中,Nesbuvir和boceprevir联合使用可导致抗性变异株出现频率降低。 |
动物实验[2]: | |
动物模型 |
尿激酶纤溶酶原激活物(uPA)/重度联合免疫缺陷(SCID)小鼠 |
剂量 |
口服给药,50 mg/kg,每天3次,持续5天 |
应用 |
用Nesbuvir处理小鼠导致HCV滴度下降2.02 ± 0.55 log10,其中一只小鼠降到了检测水平以下,然而对照组小鼠的HCV水平相对稳定(下降0.26 ± 0.16 log10)。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1]. Flint M, Mullen S, Deatly A M, et al. Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034)[J]. Antimicrobial agents and chemotherapy, 2009, 53(2): 401-411. [2]. Kneteman N M, Howe A Y M, Gao T, et al. HCV796: a selective nonstructural protein 5B polymerase inhibitor with potent anti‐hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus[J]. Hepatology, 2009, 49(3): 745-752. |
描述 | Nesbuvir是HCV NS5B RNA依赖性RNA聚合酶的选择性抑制剂。 | |||||
靶点 | HCV NS5B RNA-dependent RNA polymerase | |||||
IC50 |
质量控制和MSDS
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