Apricitabine (Synonyms: AVX754, BCH 10618, (–)-BCH 10652, (–)-dOTC, SPD-754) |
| رقم الكتالوجGC49776 |
Apricitabine (SPD754 ؛ AVX754) ، (-) enantiomer لـ 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC) ، هو مثبط للنسخة العكسية HIV-1 (RT) انتقائية للغاية وفعالة عن طريق الفم (RT) (Ki = 0.08 ميكرومتر) ، وكذلك يمنع بوليميرات الحمض النووي α و و بقيمة Ki 300 ميكرومتر و 12 ميكرومتر و 112.25 ميكرومتر على التوالي
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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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