1. Anti-infection
  2. Reverse Transcriptase
    HIV
  3. Rovafovir etalafenamide

Rovafovir etalafenamide (Synonyms: GS-9131)

Cat. No.: HY-19851
Handling Instructions

Rovafovir etalafenamide (GS-9131), a prodrug of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity.

For research use only. We do not sell to patients.

Rovafovir etalafenamide Chemical Structure

Rovafovir etalafenamide Chemical Structure

CAS No. : 912809-27-9

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Description

Rovafovir etalafenamide (GS-9131), a prodrug of the adenosine nucleotide analogue GS-9148, is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Rovafovir etalafenamide is potent and active against a variety of NRTI mutants, and shows potent anti-HIV-1 activity[1][2].

IC50 & Target[1]

HIV-1

 

reverse transcriptase

 

In Vitro

Rovafovir etalafenamide (GS-9131) shows anti-HIV-1 activity in PBMCs (EC50=3.7 nM) and MT-2 cells (EC50=150 nM). Rovafovir etalafenamide is also a potent HIV-1 inhibitor in a single-cycle infection assay with primary CD4+ T lymphocytes (EC50=24 nM). Rovafovir etalafenamide inhibits different subtypes of HIV-1 (UG-92-031 subtype A, B940374 subtype B, LJM subtype B, BR-92-025 subtype C, and UG-92-024 subtype D) clinical isolates in PBMCs with EC50s ranging from 23 to 68 nM. Rovafovir etalafenamide inhibits HIV-2 isolated in MT-2 cells (CDD77618 subtype A, CDD310248 subtype A, and CDD310319 subtype B) with EC50s ranging from 39 to 650 nM[3].

In Vivo

Rovafovir etalafenamide (GS-9131) is given orally to male beagle dogs at 3 mg/kg, it is rapidly absorbed, generating a maximum serum drug concentration (Cmax) of 2.5 μM, and is subsequently eliminated from plasma with an apparent terminal half-life (t1/2) of less than 20 min. As determined following i.v. administration, the systemic clearance of Rovafovir etalafenamide is approximately 1.4 liters/h/kg[3].

Molecular Weight

506.42

Formula

C₂₁H₂₄FN₆O₆P

CAS No.

912809-27-9

SMILES

FC([[email protected]](O1)([H])N2C3=NC=NC(N)=C3N=C2)=C[[email protected]]1OC[[email protected]](OC4=CC=CC=C4)(N[[email protected]@H](C)C(OCC)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

Rovafovir etalafenamideGS-9131GS9131GS 9131Reverse TranscriptaseHIVHuman immunodeficiency virusHIV-1subtypeprodruginfectionPBMCNRTIInhibitorinhibitorinhibit

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Rovafovir etalafenamide
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