PSI-7409
Based on 8 publication(s) in Google Scholar
PSI-7409 is the active 5'-triphosphate metabolite of Sofosbuvir (PSI-7977). Sofosbuvir (PSI-7977) is a selective and highly active nucleotide analog inhibitor of HCV.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1015073-42-3
- 分子式: C10H16FN2O14P3
- 分子量:500.16
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 PSI-7409
More- Cell. 2022 Nov 10;185(23):4347-4360.e17. [Abstract]
- Nat Commun. 2026 Jan 13;17(1):1601. [Abstract]
- Asian J Pharm Sci. 2021 Nov;16(6):772-783. [Abstract]
- J Med Chem. 2025 Jun 26;68(12):12414-12433. [Abstract]
- Antiviral Res. 2020 Mar:175:104708. [Abstract]
- Microbiol Spectr. 2022 Oct 26;10(5):e0272922. [Abstract]
- Biochem Biophys Res Commun. 2023 Jan 22:641:50-56. [Abstract]
- J Virol Methods. 2021 Dec:298:114283. [Abstract]
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
>100 μM
Compound: 2'-F,2'-C-Me-UTP
|
Inhibition of RNA polymerase 2 isolated from human HeLa cell nuclear extract assessed as decrease in incorporation of P32-alpha-CTP after 2 hrs by scintillation counting method
Inhibition of RNA polymerase 2 isolated from human HeLa cell nuclear extract assessed as decrease in incorporation of P32-alpha-CTP after 2 hrs by scintillation counting method
|
[PMID: 28595015] |
| HeLa | IC50 |
>100 μM
Compound: 3a-TP
|
Inhibition of RNA polymerase 2 in human HeLa cell nuclear extract assessed as reduction in RNA transcription by PAGE analysis
Inhibition of RNA polymerase 2 in human HeLa cell nuclear extract assessed as reduction in RNA transcription by PAGE analysis
|
[PMID: 30951311] |
体外実験
PSI-7409 inhibits the enzymatic activities of these NS5BΔ21 polymerases in a dose-dependent manner. The IC50s for PSI-7409 against GT 1b, 2a, 3a, and 4a NS5B polymerases are 1.6 μM, 2.8 μM, 0.7 μM, and 2.6 μM, respectively. PSI-7409 is a weak inhibitor of DNA Pol α (IC50=550 μM). DNA Pol β and γ are not inhibited by 1 mM PSI-7409. A significant amount of RNA product is made in the presence of 500 μM PSI-7409, about 85%[1]. In clone A cells, the levels of PSI-7409 gradually increases to a maximum concentration of about 25 μm over a period of 48 h. PSI-7409 forms at a much faster rate in primary human hepatocytes, achieving a maximum intracellular concentration of ~100 μM at 4 h and remains at that concentration for 48 h[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 1015073-42-3
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性状 Solid
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分子量 500.16
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分子式 C10H16FN2O14P3
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Color White to off-white
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SMILES
O[C@@H]([C@@](C)(F)[C@H](N1C(NC(C=C1)=O)=O)O2)[C@H]2COP(O)(OP(OP(O)(O)=O)(O)=O)=O
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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 In solvent -80°C 6 months -20°C 1 month
Publications (8)
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Journal Impact Factor
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Most Recent
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Cell
A mechanism for SARS-CoV-2 RNA capping and its inhibition by nucleotide analog inhibitors. [Abstract]2022 Nov 10;185(23):4347-4360.e17. PMID: 36335936 -
Nat Commun
2026 Jan 13;17(1):1601. PMID: 41530153 -
Asian J Pharm Sci
Liposomal remdesivir inhalation solution for targeted lung delivery as a novel therapeutic approach for COVID-19. [Abstract]2021 Nov;16(6):772-783. PMID: 34703490 -
J Med Chem
Identification of 4'-Thiouridine as an Orally Available Antiviral Agent Targeting Both RdRp and NiRAN Functions of SARS-CoV-2 Nsp12. [Abstract]2025 Jun 26;68(12):12414-12433. PMID: 40512093 -
Antiviral Res
Evaluation of sofosbuvir activity and resistance profile against West Nile virus in vitro. [Abstract]2020 Mar:175:104708. PMID: 31931104 -
Microbiol Spectr
RNA-Dependent RNA Polymerase of the Second Human Pegivirus Exhibits a High-Fidelity Feature. [Abstract]2022 Oct 26;10(5):e0272922. PMID: 35980196 -
Biochem Biophys Res Commun
Sofosbuvir and its tri-phosphate metabolite inhibit the RNA-dependent RNA polymerase activity of non-structural protein 5 from the Kyasanur forest disease virus. [Abstract]2023 Jan 22:641:50-56. PMID: 36521285 -
J Virol Methods
Surface plasmon resonance approach to study drug interactions with SARS-CoV-2 RNA-dependent RNA polymerase highlights treatment potential of suramin. [Abstract]2021 Dec:298:114283. PMID: 34534610
溶剤 & 溶解度
体外:
H2O : 50 mg/mL (99.97 mM; Need ultrasonic)
DMF : < 1 mg/mL (insoluble)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Lam AM, et al. PSI-7851, a pronucleotide of beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine monophosphate, is a potent and pan-genotype inhibitor of hepatitis C virus replication. Antimicrob Agents Chemother. 2010 Aug;54(8):3187-96. [Content Brief]
[2]. Murakami E, et al. Mechanism of activation of PSI-7851 and its diastereoisomer PSI-7977. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.9994 mL | 9.9968 mL | 19.9936 mL | 49.9840 mL |
| 5 mM | 0.3999 mL | 1.9994 mL | 3.9987 mL | 9.9968 mL | |
| 10 mM | 0.1999 mL | 0.9997 mL | 1.9994 mL | 4.9984 mL | |
| 15 mM | 0.1333 mL | 0.6665 mL | 1.3329 mL | 3.3323 mL | |
| 20 mM | 0.1000 mL | 0.4998 mL | 0.9997 mL | 2.4992 mL | |
| 25 mM | 0.0800 mL | 0.3999 mL | 0.7997 mL | 1.9994 mL | |
| 30 mM | 0.0666 mL | 0.3332 mL | 0.6665 mL | 1.6661 mL | |
| 40 mM | 0.0500 mL | 0.2499 mL | 0.4998 mL | 1.2496 mL | |
| 50 mM | 0.0400 mL | 0.1999 mL | 0.3999 mL | 0.9997 mL | |
| 60 mM | 0.0333 mL | 0.1666 mL | 0.3332 mL | 0.8331 mL | |
| 80 mM | 0.0250 mL | 0.1250 mL | 0.2499 mL | 0.6248 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.