[CAS NO. 912809-27-9] Rovafovir etalafenamide
PRODUCTS SPECIFICATIONS [912809-27-9]
DESCRIPTION [912809-27-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 506.42 |
| Molecular Formula | C21H24FN6O6P |
| SMILES | FC([C@](O1)([H])N2C3=NC=NC(N)=C3N=C2)=C[C@H]1OC[P@](OC4=CC=CC=C4)(N[C@@H](C)C(OCC)=O)=O |
Summary
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] .
IC50 & Target
|
HIV-2 |
HIV-1 |
reverse transcriptase |
In Vitro
Rovafovir etalafenamide (GS-9131) shows anti-HIV-1 activity in PBMCs (EC 50 =3.7 nM) and MT-2 cells (EC 50 =150 nM). Rovafovir etalafenamide is also a potent HIV-1 inhibitor in a single-cycle infection assay with primary CD4 + T lymphocytes (EC 50 =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 EC 50 s 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 EC 50 s ranging from 39 to 650 nM [3] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 (C max ) of 2.5 μM, and is subsequently eliminated from plasma with an apparent terminal half-life (t 1/2 ) 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] .
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03472326 | Gilead Sciences |
HIV-1-infection
|
April 3, 2018 | Phase 2 |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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.
- [2] Rai MA, Pannek S, Fichtenbaum CJ. Emerging reverse transcriptase inhibitors for HIV-1 infection. Expert Opin Emerg Drugs. 2018;23(2):149‐157.
- [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.