| Identification | Back Directory | [Name]
L-Alanine, N-[(S)-[[[(2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydro-2-furanyl]oxy]methyl]phenoxyphosphinyl]-, ethyl ester | [CAS]
912809-27-9 | [Synonyms]
GS9131
GS-9131
GS 9131
Rovafovir Etalafenamide
Rovafovir etalafenamideQ: What is
Rovafovir etalafenamide Q: What is the CAS Number of
Rovafovir etalafenamide
L-Alanine, N-[(S)-[[[(2R,5R)-5-(6-amino-9H-purin-9-yl)-4-fluoro-2,5-dihydro-2-furanyl]oxy]methyl]phenoxyphosphinyl]-, ethyl ester | [Molecular Formula]
C21H24FN6O6P | [MDL Number]
MFCD34469116 | [MOL File]
912809-27-9.mol | [Molecular Weight]
506.43 |
| Chemical Properties | Back Directory | [Boiling point ]
699.7±65.0 °C(Predicted) | [density ]
1.55±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
3.67±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Rovafovir etalafenamide (GS-9131), a proagent 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]. | [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]. | [IC 50]
HIV-2; HIV-1; reverse transcriptase | [References]
[1] Mackman RL, et al. Discovery of GS-9131: Design, synthesis and optimization of amidate prodrugs of the novel nucleoside phosphonate HIV reverse transcriptase (RT) inhibitor GS-9148. Bioorg Med Chem. 2010;18(10):3606‐3617. DOI:10.1016/j.bmc.2010.03.041
[2] Rai MA, Pannek S, Fichtenbaum CJ. Emerging reverse transcriptase inhibitors for HIV-1 infection. Expert Opin Emerg Drugs. 2018;23(2):149‐157. DOI:10.1080/14728214.2018.1474202
[3] Cihlar T, et al. Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131. Antimicrob Agents Chemother. 2008;52(2):655‐665. DOI:10.1128/AAC.01215-07 |
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