| Description | Telbivudine (NV 02B) is a Hepatitis B Virus Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of telbivudine is as a Nucleoside Reverse Transcriptase Inhibitor. The chemical classification of telbivudine is Nucleoside Analog. |
| In vivo | Telbivudine使巨噬细胞（MHV-3诱导）中肿瘤坏死因子α和白介素2水平显著增加。Telbivudine还使干扰素γ的血清水平显著增加。Telbivudine可被细胞内胸苷激酶磷酸化为活性三磷酸盐形式,其在细胞内半衰期为14 h。Telbivudine处理T细胞可增强其增殖和分泌细胞分子的能力,但对感染肝细胞的细胞毒性无影响。Telbivudine对T细胞中程序化死亡配体1表达具有抑制作用。Telbivudine分别以0.5 (N236T) 和1.0 (A181V与A194T)倍数改变,依然具有活性。菌株对拉米夫定和Telbivudine耐药性存在差异,是由于Telbivudine对耐拉米夫定的HBV菌株L180M/M204V/I突变体没有活性,但是对M204V单突变体仍然具有活性。 |
| Synonyms | NV 02B, L-Thymidine, Epavudine, 替比夫定 |
| molecular weight | 242.23 |
| Molecular formula | C10H14N2O5 |
| CAS | 3424-98-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 44 mg/mL (181.6 mM) DMSO: 50 mg/mL (206.42 mM) Ethanol: 2 mg/mL (8.25 mM), Heating is recommended. |
| References | 1. Bridges EG, et al. Antimicrob Agents Chemother, 2008, 52(7), 2521-2528. 2. Wu ZG, et al. J Viral Hepat, 2010, 17 Suppl 1, 24-33. 3. Seifer M, et al. Antiviral Res, 2009, 81(2), 147-155. |