Radalbuvir
Radalbuvir (GS-9669) is a non-nucleoside inhibitor of nonstructural protein 5B (NS5B) RNA-dependent RNA polymerase (RdRp). Radalbuvir shows strong anti-HCV potency (GT1a intrinsic EC50 = 2.9 nM, GT1b EC50 = 6 nM).
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- No. CAS: 1314795-11-3
- Fòrmula: C30H41NO6S
- Peso molecular:543.71
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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RNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
11 nM
Compound: 53, GS-9669
|
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as observed antiviral potency after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as observed antiviral potency after 72 hrs by luciferase reporter gene assay
|
[PMID: 24144213] |
| Huh-7 | EC50 |
128 nM
Compound: 53, GS-9669
|
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as plasma adjusted antiviral potency after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as plasma adjusted antiviral potency after 72 hrs by luciferase reporter gene assay
|
[PMID: 24144213] |
| Huh-7 | EC50 |
14 nM
Compound: 53, GS-9669
|
Antiviral activity against HCV genotype 1b harboring NS5B polymerase M423T mutant infected in human HuH7-Lunet cells by luciferase reporter gene assay
Antiviral activity against HCV genotype 1b harboring NS5B polymerase M423T mutant infected in human HuH7-Lunet cells by luciferase reporter gene assay
|
[PMID: 24144213] |
| Huh-7 | EC50 |
2.9 nM
Compound: 53, GS-9669
|
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as intrinsic antiviral potency after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as intrinsic antiviral potency after 72 hrs by luciferase reporter gene assay
|
[PMID: 24144213] |
| Huh-7 | EC50 |
6 nM
Compound: 53, GS-9669
|
Antiviral activity against HCV genotype 1b harboring wild type NS5B polymerase infected in human HuH7-Lunet cells by luciferase reporter gene assay
Antiviral activity against HCV genotype 1b harboring wild type NS5B polymerase infected in human HuH7-Lunet cells by luciferase reporter gene assay
|
[PMID: 24144213] |
| MT4 | CC50 |
>20 μM
Compound: 53, GS-9669
|
Cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay
Cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay
|
[PMID: 24144213] |
| MT4 | CC50 |
12138 nM
Compound: 53, GS-9669
|
Intrinsic cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay
Intrinsic cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay
|
[PMID: 24144213] |
Radalbuvir (GS-9669) shows high in vitro metabolic stability, long residence time in rats, and maintained high activity against the NS5B M423T mutation (GT1b M423T EC50 = 14 nM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1314795-11-3
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Peso molecular 543.71
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Fòrmula C30H41NO6S
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SMILES
O=C([C@@H]1CCC(C)=CC1)N([C@H]2CC[C@@](CO[C@H]3CCOC3)(O)CC2)C(C=C(C#CC(C)(C)C)S4)=C4C(O)=O
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Synonyms
GS-9669
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)