PSI-6206
Based on 3 publication(s) in Google Scholar
PSI-6206 (RO 2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibits HCV replicon with EC90 of >100 μM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.89%
- CAS. Nr.: 863329-66-2
- Formel: C10H13FN2O5
- Molecular Weight:260.22
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PSI-6206
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Biologische Aktivität
Beschreibung
IC50 & Target
EC90：>100 μM (HCV replicon)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>100 μM
Compound: 9
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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: 3
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Cytotoxicity against human HuH7 cells assessed as reduction in cell viability
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability
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[PMID: 28835346] |
| Huh-7 | EC50 |
>89 μM
Compound: 16
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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 |
>89 μM
Compound: 16
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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] |
In Vitro
PSI-6206 (RO 2433) is tested for anti-HCV activity in both a cell-based quantitative real-time RT-PCR assay and surrogate bovine viral diarrhea virus (BVDV) assays. PSI-6206 demonstrates no activity or cytoxicity in any assay[1]. The formation of the 5′-triphosphate (TP) of PSI-6130 (PSI-6130-TP) and RO2433 (RO2433-TP) increases with time and reached steady state levels at 48 h. RO2433-TP also inhibits RNA synthesis by the native HCV replicase isolated from HCV replicon cells and the recombinant HCV polymerase NS5B[2]. PSI-6206 (RO2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 863329-66-2
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Appearance Solid
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Molecular Weight 260.22
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Formel C10H13FN2O5
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Color White to light yellow
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SMILES
O=C(C=CN1[C@H]2[C@@](F)(C)[C@H](O)[C@@H](CO)O2)NC1=O
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Synonyms
RO 2433; GS-331007
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Naunyn Schmiedebergs Arch Pharmacol
Abstracts of the 83rd Annual Meeting of the German Society for Experimental and Clinical Pharmacology and Toxicology (DGPT) and the 19th Annual Meeting of the Association of the Clinical Pharmacology Germany (VKliPha) With contribution of the Arbeitsgemeinschaft für Angewandte Humanpharmakologie e. V. (AGAH). [Abstract]2017 Mar;390(Suppl 1):1-101. PMID: 28184972 -
Naunyn Schmiedebergs Arch Pharmacol
Abstracts of the 82(nd) Annual Meeting of the German Society for Experimental and Clinical Pharmacology and Toxicology (DGPT) and the 18(th) Annual Meeting of the Network Clinical Pharmacology Germany (VKliPha) in cooperation with the Arbeitsgemeinschaft für Angewandte Humanpharmakologie e.V. (AGAH). [Abstract]2016 Feb;389 Suppl 1(Suppl 1):1-104. PMID: 26852129 -
J Chromatogr B Analyt Technol Biomed Life Sci
Quantification of second generation direct-acting antivirals daclatasvir, elbasvir, grazoprevir, ledipasvir, simeprevir, sofosbuvir and velpatasvir in human plasma by UPLC-MS/MS. [Abstract]2019 Mar 15:1110-1111:15-24. PMID: 30776611
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (384.29 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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 (9.61 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.61 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Reinheit & Dokumentation
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Data Sheet (279 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Clark JL, et al. Design, Synthesis, and Antiviral Activity of 2'-Deoxy-2'-fluoro-2'-C-methyl-cytidine, a Potent Inhibitor of Hepatitis C Virus Replication. J Med Chem. 2005 Aug 25;48(17):5504-8. [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):29 [Content Brief]
[3]. Wang P, et al. An efficient and diastereoselective synthesis of PSI-6130: a clinically efficacious inhibitor of HCV NS5B polymerase. J Org Chem. 2009 Sep 4;74(17):6819-24. [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 | 3.8429 mL | 19.2145 mL | 38.4290 mL | 96.0726 mL |
| 5 mM | 0.7686 mL | 3.8429 mL | 7.6858 mL | 19.2145 mL | |
| 10 mM | 0.3843 mL | 1.9215 mL | 3.8429 mL | 9.6073 mL | |
| 15 mM | 0.2562 mL | 1.2810 mL | 2.5619 mL | 6.4048 mL | |
| 20 mM | 0.1921 mL | 0.9607 mL | 1.9215 mL | 4.8036 mL | |
| 25 mM | 0.1537 mL | 0.7686 mL | 1.5372 mL | 3.8429 mL | |
| 30 mM | 0.1281 mL | 0.6405 mL | 1.2810 mL | 3.2024 mL | |
| 40 mM | 0.0961 mL | 0.4804 mL | 0.9607 mL | 2.4018 mL | |
| 50 mM | 0.0769 mL | 0.3843 mL | 0.7686 mL | 1.9215 mL | |
| 60 mM | 0.0640 mL | 0.3202 mL | 0.6405 mL | 1.6012 mL | |
| 80 mM | 0.0480 mL | 0.2402 mL | 0.4804 mL | 1.2009 mL | |
| 100 mM | 0.0384 mL | 0.1921 mL | 0.3843 mL | 0.9607 mL |
PSI-6206 Related Classifications
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