Vidarabine是从链霉菌分离的核苷类抗生素,能抗单纯性疱疹和水痘-带状疱疹病毒。它对 HSV-1 和 HSV-2 的 IC50值分别为 9.3 μg/ml 和 11.3 μg/ml。
产品描述
Vidarabine is a nucleoside antibiotic isolated from Streptomyces antibioticus. It has some antineoplastic properties and has broad spectrum activity against DNA viruses in cell cultures and significant antiviral activity against infections caused by a variety of viruses such as the herpes viruses, the VACCINIA VIRUS and varicella zoster virus.
体外活性
Vidarabine and Acyclovir have a synergistic effect on wild type . Vidarabine is capable of inhibiting acyclovir-resistant/TK-deficient mutants of HSV and VZV, because it is phosphorylated to its active vidarabine–triphosphate form by cellular kinases and is not dependent for its activation on the viral TK. [1] Vidarabine and acyclovir (ACV) alone show a concentration-dependent inhibition of plaque formation of HSV-1 in Vero cells. Vidarabine combined with acidic protein bound polysaccharide (APBP) show synergistic effects on the plaque formation of HSV-1 in Vero cells. [2] Vidarabine acts directly on the DNA polymerase of varicella-zoster virus (VZV) and double-strand DNA viruses, including human adenoviruses. Vidarabine specifically inhibits adenovirus type 11 replication without obvious cytotoxicity in vitro. Vidarabine acts less on the synthesis of early proteins but rather on those after DNA replication. [3] Vidarabine is an antiviral drug with activity against herpes viruses, poxviruses, and certain rhabdoviruses, hepadnarviruses, and RNA tumor viruses. Vidarabine also is active against vaccinia virus both in vitro and in vivo. [4]
体内活性
Vidarabine is rapidly deaminated to 9-β-D-arabinofuranosyl hypoxanthine (Ara-Hx) as the principal metabolite. [3]
Cas No.
5536-17-4
分子式
C10H13N5O4
分子量
267.24
别名
阿糖腺苷;Arabinosyladenine;Ara-A;Adenine Arabinoside;9-β-D-Arabinofuranosyladenine;Vira-A
储存和溶解度
H2O:3 mg/mL (11.22 mM)
Ethanol:<1 mgml
DMSO:49 mg/mL (183.4 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years