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国际站:Bepirovirsen
CAS:1403787-62-1
品牌:MedChemExpress (MCE)
存储条件:Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性: Bepirovirsen 是一种针对所有 HBV 信使 RNA 的反义寡核苷酸。 Bepirovirsen 导致 HBV 衍生 RNA、HBV DNA 和病毒蛋白减少。贝匹罗韦森可用于慢性 HBV 感染的研究。贝匹罗韦森结合位点序列 (GCACTTCGCTTCACCTCTGC)[1]。
体外:Bepirovirsen(16-250 nM;16 小时)可减少 HepG2.2.15 细胞中的乙型肝炎病毒 (HBV) RNA、DNA 和病毒蛋白[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内:Bepirovirsen (22-50 mg/kg/周; 皮下注射,第 1 周每周两次,第 2-4 周每周一次) 可减少 HBV 转基因小鼠的肝脏 HBV RNA 和 DNA[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male HBV transgenic mice (Tg[HBV 1.3 genome]Chi32 against C57BL/6 background) aged 7-12 weeks and weight 18-25 g[1]. Dosage: 22, 50 mg/kg/week Administration: Injected subcutaneously twice weekly for week 1 and once weekly for weeks 2-4 Result: Dose-dependently reduced hepatic levels of HBV DNA and HBV RNA in HBV transgenic mice. Reduced levels of serum HBV DNA, serum HBsAg and serum HBeAg. Clinical Trial
参考文献:[1]. Yuen MF, et al. Safety, tolerability and antiviral activity of the antisense oligonucleotide bepirovirsen in patients with chronic hepatitis B: a phase 2 randomized controlled trial. Nat Med. 2021 Oct;27(10):1725-1734.[2]. Han K, et, al. Preclinical and Phase 1 Assessment of Antisense Oligonucleotide Bepirovirsen in Hepatitis B Virus-Transgenic Mice and Healthy Human Volunteers: Support for Clinical Dose Selection and Evaluation of Safety, Tolerability, and Pharmacokinetics of Single and Multiple Doses. Clin Pharmacol Drug Dev. 2022 Oct;11(10):1191-1202.
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