PSI-352938 (PSI-938)
(Synonyms: PSI-938) 目录号 : GC33971
PSI-352938 (PSI-938) (PSI-938) 是一种丙型肝炎病毒 (HCV) 核苷酸抑制剂。
Cas No.:1231747-17-3
Sample solution is provided at 25 µL, 10mM.
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PSI-352938 (PSI-938) is a hepatitis C virus (HCV) nucleotide inhibitor.
PSI-352938 (PSI-938) and PSI-353661 inhibit HCV genotype (GT) 1b replicon replication with 50% effective concentrations (EC50s) of 0.13±0.076 μM and 3.0±1.4 nM, respectively, and are similarly active against GT 1a and 2a replicons and infectious viruses. Metabolism of PSI-352938 and PSI-353661 generates the same 5′-triphosphate metabolite, PSI-352666, which is similarly active against NS5B polymerases from GT 1 to 4[1]. PSI-352938 (PSI-938) is a novel cyclic phosphate prodrug of β-D-2′-deoxy-2′-α-fluoro-2′-β-C-methylguanosine 5′-monophosphate that has potent activity against HCV. PSI-352938 (PSI-938) has similar activity against genotype 1a, 1b, and 2a replicons, with EC50s ranging from 0.13 to 0.20 μM and EC90 values ranging from 0.35 to 0.74 μM. PSI-352938 (PSI-938) also effectively inhibits HCV replication in the infectious virus assays: the EC50 and EC90 values are 0.28±0.083 μM and 0.63±0.018 μM, respectively, against the H77 infectious virus and 0.39±0.31 μM and 1.16±0.64 μM, respectively, against the JFH-1 infectious virus. In contrast, PSI-352938 is not active against HBV or HIV up to the highest concentration tested (EC50>100 μM)[2].
[1]. Lam AM, et al. Hepatitis C virus nucleotide inhibitors PSI-352938 and PSI-353661 exhibit a novel mechanism of resistance requiring multiple mutations within replicon RNA. J Virol. 2011 Dec;85(23):12334-42. [2]. Lam AM, et al. Inhibition of hepatitis C virus replicon RNA synthesis by PSI-352938, a cyclic phosphate prodrug of β-D-2'-deoxy-2'-α-fluoro-2'-β-C-methylguanosine. Antimicrob Agents Chemother. 2011 Jun;55(6):2566-75.
Cell experiment: | GT 1a, 1b, and 2a replicon cells are cultured in the presence of G418 (0.75 mg/mL for GT 1a, 0.25 mg/mL for GT 1b and 2a) and increasing concentrations of PSI-352938 (PSI-938) or PSI-353661 starting at their respective EC50 or EC90. As a no-compound control, replicon cells are maintained in parallel in the equivalent percent volume (0.2%) of DMSO. Cells are passaged whenever they reach ∼80% confluence and replenished with G418 medium containing fresh compound. At various passages, cells are tested for sensitivity to PSI-352938 (PSI-938) and PSI-353661. For each assay, 3-fold dilutions of test compound are added to cells in duplicate and incubated at 37°C in a humidified 5% CO2 atmosphere for 4 days. Inhibition of HCV replicon RNA replication is determined by real-time PCR (RT-PCR) using primers that anneal to the 5′ untranslated region or by measuring the levels of luminescence expressed via the firefly or Renilla luciferase reporter gene using the Bright-Glo or Renilla-Glo reagent, respectively. EC50 and EC90, the concentrations at which 50% and 90% inhibition are achieved, are determined using GraphPad Prism software. Aliquots of cells are also saved for RNA isolation, cDNA synthesis, and PCR amplification for sequencing analysis[1]. |
References: [1]. Lam AM, et al. Hepatitis C virus nucleotide inhibitors PSI-352938 and PSI-353661 exhibit a novel mechanism of resistance requiring multiple mutations within replicon RNA. J Virol. 2011 Dec;85(23):12334-42. | |
| Cas No. | 1231747-17-3 | SDF | |
| 别名 | PSI-938 | ||
| Canonical SMILES | O=P1(OC(C)C)OC[C@]2([H])[C@@]([C@@](C)(F)[C@H](N3C(N=C(N)N=C4OCC)=C4N=C3)O2)([H])O1 | ||
| 分子式 | C16H23FN5O6P | 分子量 | 431.36 |
| 溶解度 | Soluble in DMSO | 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 | 2.3182 mL | 11.5912 mL | 23.1825 mL |
| 5 mM | 0.4636 mL | 2.3182 mL | 4.6365 mL |
| 10 mM | 0.2318 mL | 1.1591 mL | 2.3182 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet