Fosdevirine
Fosdevirine (GSK2248761) is is a potent, selective, non-nucleoside reverse transcriptase inhibitor (NNRTI) of human immunodeficiency virus type 1 (HIV-1) replication with low nanomolar activity in vitro. Fosdevirine shows good activity against a broad range of HIV-1 strains, including efavirenz (HY-10572)-resistant clinical isolates.
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- No. CAS: 1018450-26-4
- Fòrmula: C20H17ClN3O3P
- Peso molecular:413.79
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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HIV-1 |
HIV-1 (K103N) |
HIV-1 (Y181C) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | EC50 |
0.001 μM
Compound: Rp-13s; IDX899
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Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| MT4 | EC50 |
0.0013 μM
Compound: Rp-13s; IDX899
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Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| MT4 | EC50 |
0.0028 μM
Compound: Rp-13s; IDX899
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Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| MT4 | EC50 |
0.0029 μM
Compound: 13s
|
Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 BH10 harboring wild type reverse transcriptase infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| MT4 | EC50 |
0.003 μM
Compound: 13s
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Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 harboring reverse transcriptase K103N mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
|
[PMID: 26804933] |
| MT4 | EC50 |
0.003 μM
Compound: 13s
|
Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| MT4 | EC50 |
0.011 μM
Compound: Rp-13s; IDX899
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Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| MT4 | EC50 |
0.0166 μM
Compound: 13s
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Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
Antiviral activity against HIV1 harboring reverse transcriptase Y181C/K103N double mutant infected in primary MT4 cells assessed as inhibition of virus-induced cytopathogenicity after 4 days by MTS assay
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[PMID: 26804933] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1018450-26-4
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Appearance Solid
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Peso molecular 413.79
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Fòrmula C20H17ClN3O3P
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Color White to off-white
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SMILES
CO[P@@](C1=C(C(N)=O)NC2=CC=C(Cl)C=C12)(C3=CC(/C=C/C#N)=CC(C)=C3)=O
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Synonyms
GSK2248761; FDV
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (269 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Castellino S, et al. Central nervous system disposition and metabolism of Fosdevirine (GSK2248761), a non-nucleoside reverse transcriptase inhibitor: an LC-MS and Matrix-assisted laser desorption/ionization imaging MS investigation into central nervous system toxicity. Chem Res Toxicol. 2013 Feb 18;26(2):241-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Fosdevirine Related Classifications
HY-14891 Related Classifications
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