1. Anti-infection
  2. HIV Reverse Transcriptase
  3. 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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Fosdevirine Chemical Structure

Fosdevirine Chemical Structure

CAS No. : 1018450-26-4

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Description

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[1].

IC50 & Target

HIV-1

 

HIV-1 (K103N)

 

HIV-1 (Y181C)

 

Cellular Effect
Cell Line Type Value Description References
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
[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
[PMID: 26804933]
MT4 EC50
0.003 μM
Compound: 13s
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
0.0166 μM
Compound: 13s
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
[PMID: 26804933]
In Vitro

Fosdevirine exhibits potent in vitro antiviral efficacy against K103N and Y181C single point mutations and was equally effective against most double mutants[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

413.79

Formula

C20H17ClN3O3P

CAS No.
SMILES

CO[P@@](C1=C(C(N)=O)NC2=CC=C(Cl)C=C12)(C3=CC(/C=C/C#N)=CC(C)=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Fosdevirine Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Fosdevirine
Cat. No.:
HY-14891
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