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My CartCAS：1190307-88-0
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1190307-88-0 |
| Name | Sofosbuvir |
| Molecular Formula | C22H29FN3O9P |
| Molecular Weight | 529.45 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 695-717-4 |
| MDL | MFCD26523124 |
| SMILES | O=C1N([C@H]2[C@]([C@H](O)[C@@H](CO[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O)O2)(C)F)C=CC(N1)=O |
| Target Point | HCV |
| Passage | Anti-infection |
| Background | Sofosbuvir is an NS5B polymerase inhibitor of HCV |
| Biological Activity | Sofosbuvir (PSI-7977) 是 HCV RNA复制抑制剂，EC50 为92 nM。[1-4] |
| In Vitro | 通过使用GT 1b(Con1)-，1a(H77)- 和2a(JFH-1)衍生的复制子和含有来自J6 GT 2a分离株的NS5B区域的GT 1b嵌合复制子，Sofosbuvir(PSI-7977)的基因型覆盖率对来自GT 2b和GT 3a的患者进行了评估，Sofosbuvir(PSI-7977)抑制具有相似EC50(16至48 nM)的这些复制子的复制，并且对含有J6 NS5B的嵌合复制子具有特异性活性(EC50 = 4.7 nM)。 Sofosbuvir(PSI-7977)抑制克隆A(GT 1b)野生型和S282T复制子，EC90值分别为0.42和7.8μM[2]。在克隆A复制子测定中，Sofosbuvir(PSI-7977)产生抗HCV活性，EC90值为0.42μM[3]。 |
| Cell Experiment | 将克隆A细胞以约5×10 6个细胞/瓶接种到含有100IU/mL青霉素/100μg/ mL链霉素和10％胎牛血清的Dulbecco's改良Eagle培养基(DMEM)中的T75烧瓶中。类似地，将人原代肝细胞以约5×10 6个细胞/瓶接种在细胞平板培养基中的T75烧瓶中。孵育过夜以使细胞附着后，将细胞与50μMPSI-7851，PSI-7976或Sofosbuvir(PSI-7977)在新鲜培养基中培养用于克隆A细胞或在用于原代肝细胞的细胞维持培养基中培养至多24 h在37℃，5％CO 2气氛中。当在研究中使用放射性标记的PSI-7851时，应用相同的程序，除了将每孔1×10 6个细胞接种到6孔板中，并将细胞与5μM[3H] PSI-7851一起孵育。在选定的时间，除去培养基，用冷的磷酸盐缓冲盐水(PBS)洗涤细胞层。胰蛋白酶消化后，计数细胞并以1，200rpm离心5分钟。将细胞沉淀悬浮在1mL冷的60％甲醇中，并在-20℃下温育过夜。将样品以14，000rpm离心5分钟，收集上清液并使用SpeedVac浓缩器干燥，并储存在-20℃直至通过高效液相色谱(HPLC)分析。将残留物悬浮于100μL水中，并将50μL等分试样注入HPLC [1]。 |
| Data Literature Source | [1]. Murakami E，et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977.J Biol Chem. 2010 Nov 5;285(45):34337-47. [2]. Lam AM，et al. Genotype and subtype profiling of PSI-7977 as a nucleotide inhibitor of hepatitis C virus. Antimicrob Agents Chemother. 2012 Jun;56(6):3359-68. [3]. Sofia MJ，et al. Discovery of a β-d-2'-deoxy-2'-α-fluoro-2'-β-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J Med Chem. 2010 Oct 14;53(19):7202-18. [4]. Zhang X，et al. Discovery and evolution of aloperine derivatives as a new family of HCV inhibitors with novel mechanism. Eur J Med Chem. 2018 Jan 1;143:1053-1065. |
| Unit | Bottle |
| Specification | 5mg 10mg 20mg |
是一种 HCV的NS5B polymerase抑制剂
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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