Name | 3'-azido-2',3'-dideoxyuridine |
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Synonyms |
AzddU
3'-Azido-2',3'-dideoxyuridine Uridine, 3'-azido-2',3'-dideoxy- 2',3'-Dideoxy-3'-azidouridine 3'-Azido-2',3'-dideoxy-D-uridine navuridine 3'-Az-ddU CS-87 |
Description | 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]. |
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Related Catalog | |
Target |
HIV |
In Vitro | 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]。< br/>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]. IV (25 mg/kg) IV (100 mg/kg) PO (25 mg/kg) PO (100 mg/kg) Cmax (μg/mL) 9.2±1.9 41±15 Tmax (h) 0.38±0.13 0.63±0.22 AUC (μg/mL∗h) 19±1.2 156±7.0 12±0.54 70±13 CLT (L/h/kg) 1.4±0.2 0.70±0.09 CLR (L/h/kg) 0.90±0.27 0.43±0.12 t1/2 (h) 0.5±0.0 0.68±0.1 1.0±0.3 1.1±0.4 Vss (L/kg) 0.78±0.26 0.34±0.11 F (%) 60 46 Animal Model: Adult male Sprague-Dawley rats (300-400 g)[3] Dosage: 25, 100 mg/kg Administration: Intravenous bolus injection or oral gavage (Pharmacokinetic Analysis) Result: The oral bioavailability estimates of 3′-Azido-2′,3′-dideoxyuridine at doses of 25 and 100 mg/kg averaged 53%. |
References |
Density | 1.357 g/cm |
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Melting Point | 161-163ºC |
Molecular Formula | C9H11N5O4 |
Molecular Weight | 253.215 |
Exact Mass | 253.081100 |
PSA | 134.07000 |
LogP | -1.12 |
Storage condition | −20°C |
Hazard Codes | Xn |
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WGK Germany | 3 |
HS Code | 2934999090 |
Precursor 10 | |
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DownStream 8 | |
HS Code | 2934999090 |
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Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |