PSI-353661
PSI-353661 (GS-558093) is a purine nucleotide NS5B polymerase inhibitor against HCV infection. PSI-353661 shows EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons of HCV. PSI-353661 can produce high concentrations of the active triphosphate in primary human hepatocytes.
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- CAS No.: 1231747-08-2
- Formule: C24H32FN6O8P
- Masse moléculaire:582.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
NS5B polymerase[3]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CCRF-CEM | CC50 |
>100 μM
Compound: 23
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Cytotoxicity against human CEM cells after 96 hrs by MTS assay
Cytotoxicity against human CEM cells after 96 hrs by MTS assay
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[PMID: 24900291] |
| HepG2 | CC50 |
62 μM
Compound: 23
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Cytotoxicity against human HepG2 cells after 96 hrs by MTS assay
Cytotoxicity against human HepG2 cells after 96 hrs by MTS assay
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[PMID: 24900291] |
| Huh-7 | CC50 |
>100 μM
Compound: 23
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Cytotoxicity against human HuH7 cells after 96 hrs by MTS assay
Cytotoxicity against human HuH7 cells after 96 hrs by MTS assay
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[PMID: 24900291] |
In Vitro
PSI-353661 exhibits strong inhibition of HCV in the cell-based replicon assay, with EC90s of 8 nM and 11 nM for wild type and S282T resistant replicons[1].
PSI-353661 (24 h) produces high concentrations of (0.44 mM) triphosphate (TP) level in primary human hepatocytes[1].
PSI-353661 (4 days) inhibits viral replication with EC50 and EC90 value of 0.0030 μM and 0.0085 μM for genotype 1b replicon cells[2].
PSI-353661 (8 days) shows little cytotoxicity in Huh7, HepG2, BxPC3, and CEM cells, with IC50 more than 80 μM[2].
PSI-353661 (8-160 nM, 2 weeks) clears HCV replicon RNA and prevents viral rebound[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Human hepatocyte chimeric mice infected with HCV
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Dosage:50 mg/kg, together with 400 mg/kg of Telaprevir
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Administration:Oral administration (p.o.)
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Result:Achieved sustained eradication of the mutant virus or the end-of-treatment response.
Reduced serum levels of HCV RNA.
Chemical Information
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CAS No. 1231747-08-2
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Masse moléculaire 582.52
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Formule C24H32FN6O8P
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SMILES
COC1=NC(N)=NC2=C1N=CN2[C@@H]([C@@](F)(C)[C@@H]3O)O[C@@H]3CO[P@@](N[C@@H](C)C(OC(C)C)=O)(OC4=CC=CC=C4)=O
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Synonyms
GS-558093
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Wonsuk Chang, et al. Discovery of PSI-353661, a Novel Purine Nucleotide Prodrug for the Treatment of HCV Infection. ACS Med Chem Lett. 2010 Dec 17;2(2):130-5. [Content Brief]
[2]. Furman PA, et al. Activity and the metabolic activation pathway of the potent and selective hepatitis C virus pronucleotide inhibitor PSI-353661. Antiviral Res. 2011 Aug;91(2):120-32. [Content Brief]
[3]. Yugo Kai, et al. Emergence of hepatitis C virus NS5A L31V plus Y93H variant upon treatment failure of daclatasvir and asunaprevir is relatively resistant to ledipasvir and NS5B polymerase nucleotide inhibitor GS-558093 in human hepatocyte chimeric mice. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PSI-353661 Related Classifications
HY-14391 Related Classifications
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