R-7128
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.
R-7128(Mericitabine)是丙型肝炎病毒(HCV)NS5B RNA依赖性RNA聚合酶的选择性核苷类似物抑制剂。
丙型肝炎病毒(HCV)是一种有包膜的单链RNA病毒。病毒RNA经由HCV的RNA依赖性RNA聚合酶在宿主细胞中复制,引起丙型肝炎和某些癌症淋巴瘤。
R-7128,一种三磷酸核苷酸类似物,是HCV聚合酶NS5B的底物。R-7128插入到新生HCV RNA,通过RNA聚合酶NS5B大幅降低RNA延伸的效率,导致新生RNA产物的终止。实验表明,R-7128能够抑制HCV RNA的体外合成[1]。
给予32名HCV基因型1感染患者750 mg或1500 mg的R-7128,每日一次(QD)或两次(BID),持续14天,同时,经常测定HCV RNA水平。R-7128治疗组中HCV RNA的初始下降通常较α-干扰素或蛋白酶抑制剂治疗组中的慢,但12名患者显现出一种新型的HCV RNA动力学模式,抑制病毒繁殖的效率随着时间的推移逐渐升高,直到达到其最终值。BID剂量下的最终值高(平均750 mg和1500 mg:98.0%和99.8%,P = 0.018),并显著地比QD剂量下患者的最终值高(平均QD对BID:90%比99%)(P<10^-7)[2]。
参考文献:
[1] Ma H et al. , Characterization of the metabolic activation of Hepatitis C virus nucleoside inhibitor β-D-2′-Deoxy-2′-fluoro-2′-C-methylcytidine (PSI-6130) and identification of a novel active 5′-Triphosphate species. J Biol Chem. 2007, 282(41): 29812-20.
[2] Guedj J et al. , Hepatitis C viral kinetics with the nucleoside polymerase inhibitor mericitabine (RG7128). Hepatology. 2012, 55(4): 1030-1037.
Storage | Store at -20°C |
M.Wt | 399.41 |
Cas No. | 940908-79-2 |
Formula | C18H26FN3O6 |
Synonyms | RG 7128; Mericitabine; PSI 6130 diisobutyrate |
Solubility | Soluble in DMSO |
Chemical Name | [(2R,3R,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-4-fluoro-4-methyl-3-(2-methylpropanoyloxy)oxolan-2-yl]methyl 2-methylpropanoate |
SDF | Download SDF |
Canonical SMILES | CC(C)C(=O)OCC1C(C(C(O1)N2C=CC(=NC2=O)N)(C)F)OC(=O)C(C)C |
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。 |
描述 | R-7128(Mericitabine)是丙型肝炎病毒(HCV)NS5B RNA依赖性RNA聚合酶的选择性核苷类似物抑制剂。 | |||||
靶点 | HCV | |||||
IC50 |