产品说明书

Telbivudine

Print
Chemical Structure| 3424-98-4 同义名 : NV 02B;Epavudine;Tyzeka;LDT 600;β-L-Thymidine;L-Deoxythymidine;2'-deoxy-L-Thymidine;L-Thymidine
CAS号 : 3424-98-4
货号 : A158594
分子式 : C10H14N2O5
纯度 : 98%
分子量 : 242.229
MDL号 : MFCD02683612
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(206.42 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 30 mg/mL(123.85 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 Telbivudine, an orally active thymidine nucleoside analog, is a potent antiviral inhibitor of hepatitis B virus (HBV) replication[3]. Telbivudine reverses B19V-induced dysregulation of BIRC3 (Baculoviral Inhibitor of apoptosis Repeat-Containing protein 3), thus, intervening in the apoptosis pathway and protecting susceptible cells from cell death[4]. Telbivudine given for 4 weeks resulted in an 8-log reduction of woodchuck hepatitis virus DNA, and a 3.8-log reduction of hepatitis B virus DNA in human. After 52 weeks of telbivudine treatment there was an approximate 6-log reduction of hepatitis B virus DNA levels, hepatitis B virus DNA became undetectable by PCR assay in 61% of patients. Its antiviral efficacy is significantly better than lamivudine[5]. In vitro assays revealed that telbivudine treatment induced TGF-β1 expression in human macrophagic cells. Telbivudine treatment enhanced the proportion of serum IgG-Fc agalactosylation in cirrhotic patients, which was associated with enhanced levels of TGF-β1 and IgG[6]. Telbivudine exerts endothelial-protective effects in B19V-infected endothelial cells and improves chronic myocarditis associated with B19V transcriptional activity[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.64mL

4.13mL

2.06mL

41.28mL

8.26mL

4.13mL

参考文献

[1]Wu ZG, Yan WM, et al. Telbivudine preserves T-helper 1 cytokine production and downregulates programmed death ligand 1 in a mouse model of viral hepatitis. J Viral Hepat. 2010 Mar;17 Suppl 1:24-33.

[2]Bridges EG, Selden JR, Luo S. Nonclinical safety profile of telbivudine, a novel potent antiviral agent for treatment of hepatitis B. Antimicrob Agents Chemother. 2008 Jul;52(7):2521-8.

[3]Kim JW, Park SH, Louie SG. Telbivudine: a novel nucleoside analog for chronic hepatitis B. Ann Pharmacother. 2006 Mar;40(3):472-8

[4]Zobel T, Bock CT, Kühl U, Rohde M, Lassner D, Schultheiss HP, Schmidt-Lucke C. Telbivudine Reduces Parvovirus B19-Induced Apoptosis in Circulating Angiogenic Cells. Viruses. 2019 Mar 6;11(3):227

[5]Yuen MF, Lai CL. Telbivudine: an upcoming agent for chronic hepatitis B. Expert Rev Anti Infect Ther. 2005 Aug;3(4):489-94

[6]Ho CH, Chang TT, Chien RN. Telbivudine on IgG-associated hypergammaglobulinemia and TGF-β1 hyperactivity in hepatitis B virus-related liver cirrhosis. PLoS One. 2019 Nov 26;14(11):e0225482

[7]Van Linthout S, Elsanhoury A, Klein O, Sosnowski M, Miteva K, Lassner D, Abou-El-Enein M, Pieske B, Kühl U, Tschöpe C. Telbivudine in chronic lymphocytic myocarditis and human parvovirus B19 transcriptional activity. ESC Heart Fail. 2018 Oct;5(5):818-829