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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 Chemical Structure Rovafovir etalafenamide(Synonyms: GS-9131)](http://www.fluoroprobe.com/wp-content/uploads/2022/05/hy-19851.gif)
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]. |
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IC50 & Target[1] |
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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. |
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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. |
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Clinical Trial |
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分子量 |
506.42 |
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Formula |
C21H24FN6O6P |
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CAS 号 |
912809-27-9 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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