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Rovafovir etalafenamide

CAS No. : 912809-27-9

MCE 站：Rovafovir etalafenamide

产品活性：Rovafovir etalafenamide (GS-9131) 是腺苷核苷酸类似物 GS-9148 的前药，是一种口服活性核苷逆转录酶抑制剂 (NRTI)。Rovafovir etalafenamide 对多种 NRTI 突变体有效且具有活性，并显示出有效的抗 HIV-1 活性。

研究领域：Anti-infection

作用靶点：Reverse Transcriptase  |  HIV

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.

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.

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