Rovafovir etalafenamide(Synonyms: GS-9131)

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Rovafovir etalafenamide (Synonyms: GS-9131)

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。

Rovafovir etalafenamide(Synonyms: GS-9131)

Rovafovir etalafenamide Chemical Structure

CAS No. : 912809-27-9

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生物活性

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

 

体外研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

506.42

Formula

C21H24FN6O6P
CAS 号

912809-27-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

  • [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.

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