Bioactivity | 3′-Azido-2′,3′-dideoxyuridine (AzdU) is a nucleoside analog of Zidovudine (HY-17413). 3′-Azido-2′,3′-dideoxyuridine is a potent inhibitor of human immunodeficiency virus (HIV) replication in human peripheral blood mononuclear cells (PBMC) with limited toxicity for human bone marrow cells (BMC)[1][2][3]. | |||||||||
Invitro | 3'-Azido-2',3'-dideoxyuridine 抑制感染 HIV-1 的 PBMC 中的 HIV 复制,中位有效浓度为 0.18-0.46 μM[2]。3'-Azido-2',3'-dideoxyuridine 抑制人类 T 细胞系 MT-4 和 ATH8 中 HIV 介导的细胞病变效应,中位有效浓度为 0.4 µM[3]。3'-Azido-2',3'-dideoxyuridine 依次被细胞激酶磷酸化为单磷酸、二磷酸和三磷酸代谢物[3]。 | |||||||||
In Vivo | 3′-Azido-2′,3′-dideoxyuridine (25-100 mg/kg, 静脉注射或者灌胃,一次)具有良好的药代动力学特征[3]。Pharmacokinetic Parameters of 3′-Azido-2′,3′-dideoxyuridine in male Sprague-Dawley rats[3]. | |||||||||
Name | 3′-Azido-2′,3′-dideoxyuridine | |||||||||
CAS | 84472-85-5 | |||||||||
Formula | C9H11N5O4 | |||||||||
Molar Mass | 253.21 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [1]. Zhu Z, et al. Cellular metabolism of 3'-azido-2',3'-dideoxyuridine with formation of 5'-O-diphosphohexose derivatives by previously unrecognized metabolic pathways for 2'-deoxyuridine analogs. Mol Pharmacol. 1990 Dec;38(6):929-38. [2]. Chu CK, et al. Structure-activity relationships of pyrimidine nucleosides as antiviral agents for human immunodeficiency virus type 1 in peripheral blood mononuclear cells. J Med Chem. 1989 Mar;32(3):612-7. [3]. Kong L, et al. Pharmacokinetic evaluation of 3'-azido-2', 3'-dideoxyuridine-5'-O-valinate-hydrochloride as a prodrug of the anti-HIV nucleoside 3'-azido-2', 3'-dideoxyuridine. Antivir Chem Chemother. 2003 Sep;14(5):263-70. |