常用名 | 替比夫定 | CAS号 | 3424-98-4 |
---|---|---|---|
价格 | ¥需询单/1mg | 纯度 | 98.0% |
备货期 | 3天 | 库存 | 现货 |
产品详情(用途,包装等)
用途: Telbivudine, a specific inhibitor of hepatitis B virus (HBV) replication, is an antiviral drug used in the treatment of hepatitis B infection.Target: HBVTelbivudine is an antiviral drug used in the treatment of hepatitis B infection. It is marketed by Swiss pharmaceutical company Novartis under the trade names Sebivo (Europe) and Tyzeka (United States). Clinical trials have shown it to be significantly more effective than lamivudine or adefovir, and less likely to cause resistance. Telbivudine is a synthetic thymidine nucleoside analogue, it is the L-isomer of thymidine. It is taken once daily.Telbivudine is a potent antiviral that provides effective and sustained viral suppression in patients with compensated CHB. In clinical trials, treatment outcomes were improved significantly more with telbivudine 600 mg once daily than with lamivudine 100 mg or adefovir 10 mg once daily, and telbivudine-treated patients had significantly less viral resistance than lamivudine-treated patients. Telbivudine is associated with a medium genetic barrier to resistance and, as patients with undetectable HBV DNA levels have significantly improved outcomes, it is recommended that HBV DNA levels are monitored at week 24 (and 6 monthly thereafter), with the addition of a nucleoside/nucleotide analogue without cross resistance (such as adefovir dipivoxil) if viraemia is present to reduce the risk of resistance (Roadmap concept). Telbivudine was generally well tolerated in clinical trials for periods of up to 4 years, and has a similar tolerability profile to that of lamivudine. 作用: 1.作用机制:替比夫定为天然胸腺嘧啶脱氧核苷的自然L-对映体,是人工合成的胸腺嘧啶脱氧核苷类抗乙肝病毒(HBV)DNA多聚酶药物。 替比夫定在细胞激酶的作用下被磷酸化为有活性的代谢产物--腺苷,腺苷的细胞内半衰期为14小时。替比夫定5'-腺苷通过与HBV中自然底物胸腺嘧啶5'-腺苷竞争,从而抑制HBVDNA多聚酶的活性;通过整和到HBVDNA中造成乙肝病毒(HBV)DNA链延长终止,从而抑制乙肝病毒的复制。 替比夫定同时抑制乙肝病毒(HBV)DNA第一链(EC50value=1.3±1.6μ 物理化学性质: CAS号:3424-98-4 常用中文名:替比夫定 常用英文名:Telbivudine 分子式:C10H14N2O5 分子量:242.229 密度:1.5±0.1 g/cm3 沸点:N/A 熔点:188-190ºC 闪点:N/A 储存条件:2-8°C |