TMC647055 Choline salt
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.
TMC647055是丙型肝炎病毒NS5B聚合酶的有效选择性非核苷抑制剂,EC50值为82 nM [1].
丙型肝炎病毒(HCV) NS5B聚合酶是RNA依赖性的RNA聚合酶,负责病毒复制,在HCV生命周期中发挥重要作用.HCV是形成慢性肝病和急性肝炎的主要原因,最终导致肝衰竭\肝硬化和肝细胞癌[1].
TMC647055是一种选择性和细胞渗透的HCV NS5B抑制剂.在RNA聚合酶引物依赖的转录实验中,TMC647055抑制HCV NS5B聚合酶,IC50值为34 nM.在Huh7-Luc细胞系中,TMC647055抑制基因型1b复制子的复制,荧光素酶读出和定量RT-PCR读出测定的EC50值分别为77和139 nM.在除基因型2b之外的所有基因型中,TMC647055与NS5B具有较高亲和力,中位值KD值小于35 nM.在Huh7-Luc复制子细胞中,750 nM的TMC647055减少30个细胞集落的形成.此外,1.5 μM和3.75 μM 的TMC647055降低HCV复制子RNA含量[2][3].
参考文献：
[1]. Vendeville S, Lin TI, Hu L, et al. Finger loop inhibitors of the HCV NS5b polymerase. Part II. Optimization of tetracyclic indole-based macrocycle leading to the discovery of TMC647055. Bioorg Med Chem Lett, 2012, 22(13): 4437-4443.
[2]. Devogelaere B, Berke JM, Vijgen L, et al. TMC647055, a potent nonnucleoside hepatitis C virus NS5B polymerase inhibitor with cross-genotypic coverage. Antimicrob Agents Chemother, 2012, 56(9): 4676-4684.
[3]. Cummings MD, Lin TI, Hu L, et al. Discovery and early development of TMC647055, a non-nucleoside inhibitor of the hepatitis C virus NS5B polymerase. J Med Chem, 2014, 57(5): 1880-1892.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 727.91 |
| Cas No. | 1204416-97-6 |
| Formula | C37H53N5O8S |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥72.8 mg/mL in DMSO with gentle warming |
| SDF | Download SDF |
| Canonical SMILES | OCC[N+](C)(C)C.COC1=CC2=C(C3=C(C4=CC=C(C(NS(N(C)CCOCCN(C)C5=O)(=O)=O)=O)C=C4N3CC5=C2)C6CCCCC6)C=C1.[OH-] |
| 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。 |
质量控制和MSDS
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化学结构
