Apricitabine (Synonyms: AVX754, BCH 10618, (–)-BCH 10652, (–)-dOTC, SPD-754) |
| カタログ番号GC49776 |
2'-デオキシ-3'-オキサ-4'-チオシチジン (dOTC) の (-) エナンチオマーであるアプリシタビン (SPD754; AVX754) は、高度に選択的で経口的に活性な HIV-1 逆転写酵素 (RT) 阻害剤です (Ki= 0.08 μM)、DNA ポリメラーゼ α、β、γ をそれぞれ 300 μM、12 μM、112.25 μM の Ki 値で阻害します 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 160707-69-7
Sample solution is provided at 25 µL, 10mM.
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Apricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) and derivative of 2’-deoxycytidine .1 It is phosphorylated intracellularly to its active form, apricitabine-5’-triphosphate, which competes with a monophosphate form for binding to HIV-1 reverse transcriptase and incorporation into the nascent viral DNA, inducing chain termination and HIV-1 replication. Apricitabine reduces HIV-1 infectivity in MT-4 and U937 cells (IC50s = 2.8 and 0.4 µM, respectively), as well as in isolated human cord blood mononuclear cells (CBMCs; IC50 = 0.4 µM).2
1.Cox, S., and Southby, J.Apricitabine--a novel nucleoside reverse transcriptase inhibitor for the treatment of HIV infection that is refractory to existing drugsExpert Opin. Investig. Drugs18(2)199-209(2009) 2.Mansour, T.S., Jin, H., Wang, W., et al.Structure-activity relationships among a new class of antiviral heterosubstituted 2′,3′-dideoxynucleoside analoguesNucleos. Nucleot.14(3-5)627-635(1995)
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