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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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: 1314795-11-3
- 分子式: C30H41NO6S
- 分子量:543.71
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
DNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
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RNA Polymerase |
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Cell Line
|
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 |
化学情報
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CAS 番号 1314795-11-3
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分子量 543.71
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分子式 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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別名
GS-9669
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輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)