PSI-6130
(Synonyms: 2'-去氧-2'-氟-2'-C-甲基胞苷,R 1656) 目录号 : GC37028
An HCV NS5B inhibitor
Cas No.:817204-33-4
Sample solution is provided at 25 µL, 10mM.
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PSI-6130 is a nucleoside inhibitor of the NS5B RNA polymerase of hepatitis C virus (HCV; Ki = 4.3 ?M).1 It inhibits HCV genotype 1b (GT-1b) Con1 and GT-1a H77 viral replication in Huh7 replicon cells using a luciferase-based assay (EC50s = 0.51 and 0.30 ?M, respectively). PSI-6130 also inhibits replication of HCV GT-1b and GT-1a replicons from clinical isolates, with EC50 values ranging from 0.60 to 1.41 ?M, and 0.20 to 0.43 ?M, respectively, in the same assay. It has little or no activity against West Nile Virus (WNV), Dengue type 2 virus (DV), human immunodeficiency virus (HIV), or hepatitis B virus (HBV; EC90s = 46.3, >100, >100, and >10 ?M, respectively).2
1.Murakami, E., Bao, H., Ramesh, M., et al.Mechanism of activation of β-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymeraseAntimicrob. Agents Chemother.51(2)503-509(2007) 2.Stuyver, L.J., McBrayer, T.R., Tharnish, P.M., et al.Inhibition of hepatitis C replicon RNA synthesis by β-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine: A specific inhibitor of hepatitis C virus replicationAntivir. Chem. Chemother.17(2)79-87(2006)
Kinase experiment: | The inhibition potency of compounds with respect to the RdRp activity of recombinant NS5B570-BK, NS5B570-Con1, and NS5B570-H77 proteins is determined by measuring the incorporation of radiolabeled NMP into acid-insoluble RNA products by use of a complement strand of internal ribosomal entry site (cIRES) RNA template. Briefly, 50% inhibitory concentration (IC50) determinations are carried out using 200 nM in vitro-transcribed cIRES RNA template, 1 μCi of tritiated UTP (42 Ci/mmol), 500 μM ATP, 500 μM GTP, 1 μM CTP, 1× TMDN buffer (40 mM Tris-HCl [pH 8.0], 4 mM MgCl2, 4 mM dithiothreitol, 40 mM NaCl), and 200 nM enzyme. The inhibition potency of compounds with respect to the RdRp activity of NS5B570-S282T-Con1 is determined under GT-1b assay conditions as. NS5B570-BK and NS5B570-Con1 enzymes are used as controls. The final reaction volume is 50 μL under all assay conditions. All reactions contain a final 10% dimethyl sulfoxide. Km and Ki values are measured. |
References: [1]. Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. | |
| Cas No. | 817204-33-4 | SDF | |
| 别名 | 2'-去氧-2'-氟-2'-C-甲基胞苷,R 1656 | ||
| Canonical SMILES | O=C1N=C(C=CN1[C@@H]([C@@](C)([C@@H]2O)F)O[C@@H]2CO)N | ||
| 分子式 | C10H14FN3O4 | 分子量 | 259.23 |
| 溶解度 | DMSO: ≥ 50 mg/mL (192.88 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.8576 mL | 19.2879 mL | 38.5758 mL |
| 5 mM | 0.7715 mL | 3.8576 mL | 7.7152 mL |
| 10 mM | 0.3858 mL | 1.9288 mL | 3.8576 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet