PSI-6130
Based on 2 publication(s) in Google Scholar
PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC50 of 0.6 μM.
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- 純度: 99.90%
- CAS 番号: 817204-33-4
- 分子式: C10H14FN3O4
- 分子量:259.24
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 PSI-6130
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生物活性
IC50: 0.6 μM (HCV replication)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>100 μM
Compound: 1
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Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay
Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay
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[PMID: 16107149] |
| Huh-7 | CC50 |
>100 μM
Compound: PSI-6130
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Cytotoxicity against human HuH7 cells
Cytotoxicity against human HuH7 cells
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[PMID: 18285474] |
| Huh-7 | CC50 |
>50 μM
Compound: 1, PSI-6130
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Cytotoxicity against human HuH7 cells by MTS assay
Cytotoxicity against human HuH7 cells by MTS assay
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[PMID: 20580554] |
| Huh-7 | CC50 |
>98 μM
Compound: 9a, PSI-6130
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Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay
Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay
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[PMID: 24345201] |
| Huh-7 | CC50 |
>98.4 μM
Compound: 2, PSI-6130
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Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay
Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay
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[PMID: 21033671] |
| Huh-7 | EC50 |
0.6 μM
Compound: 17
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Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay
Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay
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[PMID: 25650256] |
| Huh-7 | EC50 |
0.61 μM
Compound: PSI-6130
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Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay
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[PMID: 18285474] |
| Huh-7 | EC50 |
1.9 μM
Compound: 2, PSI-6130
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Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay
Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay
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[PMID: 21033671] |
| Huh-7 | EC50 |
1.9 μM
Compound: 9a, PSI-6130
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Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay
Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay
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[PMID: 24345201] |
| Huh-7 | EC50 |
2.3 μM
Compound: 17
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Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay
Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay
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[PMID: 25650256] |
| Huh-7 | EC50 |
4.5 μM
Compound: PSI-6130
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Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days
Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days
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[PMID: 27994763] |
| MT4 | CC50 |
>98.4 μM
Compound: 2, PSI-6130
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Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay
Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay
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[PMID: 21033671] |
PSI-6130 exhibits potent and specific inhibitory activity against HCV RNA replication mediated by the NS5B polymerase. Both PSI-6130 inhibit HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA replication, with mean EC50 values of 0.51 and 0.30 μM, respectively. PSI-6130 inhibits 40% human serum with EC50 of 0.51 μM[1]. PSI-6130 inhibits HCV replication with a mean IC50 of 0.6 μM, PSI-6130-TP inhibits HCV replicase with a mean IC50 of 0.34 μM. PSI-6130-TP inhibits recombinant HCV Con1 NS5B on a heteropolymeric RNA template derived from the 3′-end of the negative strand of the HCV genome with an IC50 of 0.13 μM and Ki of 0.023 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 817204-33-4
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性状 Solid
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分子量 259.24
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分子式 C10H14FN3O4
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Color White to off-white
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SMILES
O=C1N=C(C=CN1[C@@H]([C@@](C)([C@@H]2O)F)O[C@@H]2CO)N
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別名
R 1656
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Antiviral Res
Antiviral candidates against the hepatitis E virus (HEV) and their combinations inhibit HEV growth in in vitro. [Abstract]2019 Oct;170:104570. PMID: 31362004 -
ACS Infect Dis
Targeting the Rift Valley Fever Virus Polymerase: Resistance Mechanisms and Structural Insights. [Abstract]2025 Oct 30. PMID: 41166549
溶剤 & 溶解度
DMSO : 25 mg/mL (96.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[2]. Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.8575 mL | 19.2874 mL | 38.5747 mL | 96.4369 mL |
| 5 mM | 0.7715 mL | 3.8575 mL | 7.7149 mL | 19.2874 mL | |
| 10 mM | 0.3857 mL | 1.9287 mL | 3.8575 mL | 9.6437 mL | |
| 15 mM | 0.2572 mL | 1.2858 mL | 2.5716 mL | 6.4291 mL | |
| 20 mM | 0.1929 mL | 0.9644 mL | 1.9287 mL | 4.8218 mL | |
| 25 mM | 0.1543 mL | 0.7715 mL | 1.5430 mL | 3.8575 mL | |
| 30 mM | 0.1286 mL | 0.6429 mL | 1.2858 mL | 3.2146 mL | |
| 40 mM | 0.0964 mL | 0.4822 mL | 0.9644 mL | 2.4109 mL | |
| 50 mM | 0.0771 mL | 0.3857 mL | 0.7715 mL | 1.9287 mL | |
| 60 mM | 0.0643 mL | 0.3215 mL | 0.6429 mL | 1.6073 mL | |
| 80 mM | 0.0482 mL | 0.2411 mL | 0.4822 mL | 1.2055 mL |
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