阿普西他滨 (SPD754; AVX754) 是 2'-deoxy-3'-oxa-4'-thiocytidine (dOTC) 的 (-) 对映异构体，是一种高选择性和口服活性的 HIV-1 逆转录酶 (RT) 抑制剂 (Ki= 0.08 μM)，以及抑制 DNA 聚合酶 α、β 和 γ，Ki 值分别为 300 μM、12 μM 和 112.25 μM。
货号:ajcx26478
CAS:160707-69-7
分子式:C8H11N3O3S
分子量：229.3
溶解度:DMSO: soluble
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Apricitabine is a nucleoside reverse transcriptase inhibitor (NRTI) and derivative of 2’-deoxycytidine .¹It 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)