Telbivudine Inhibitor CAS No. 3424-98-4

Cat. No.	Name	Size	Price
KI0967	Telbivudine	250 mg	$1228.5
	Telbivudine	1 g	$1960
	Telbivudine	5 g	$7840

Chemical Characteristic

Product Name	Telbivudine
Synonyms	Tyzeka, Sebivo
CAS No.	3424-98-4
Molecular Weight	242.23
Formula	C₁₀H₁₄N₂O₅
Chemical Structure

Biological activities

Telbivudine is an antiviral drug used in the treatment of hepatitis B infection. Telbivudine is significantly more effective than lamivudine or adefovir, and less likely to cause resistance. Telbivudine is phosphorylated by intracellular thymidine kinases to the active triphosphate form, which has an intracellular half-life of 14 hours.^[1] In enzymatic assays, telbivudine inhibits the woodchuck hepatitis virus DNA polymerase with an IC50 value of 240 nM.^[2] In hepatoma cell culture assays, telbivudine inhibits HBV production with an IC50 value ranging from 50 to 650 nM, depending on the cell type, growth conditions, and the assay used. Telbivudine is active against duck HBV in primary duck hepatocytes with an IC50 value of 180 nM.^[3] In a mouse model of MHV-3-induced hepatitis, telbivudine preserves T-helper 1 cytokine production and downregulates programmed death ligand 1.^[4]

Protocols

In vivo: Telbivudine is dissolved in DMSO. ^[5]

References

[1] Hernandez-Santiago B, et al. Pharmacology of beta-L-thymidine and beta-L-2'-deoxycytidine in HepG2 cells and primary human hepatocytes: relevance to chemotherapeutic efficacy against hepatitis B virus. Antimicrob Agents Chemother. 2002, 46(6): 1728-1733. [2] Bryant ML, et al. Antiviral L-nucleosides specific for hepatitis B virus infection. ? Antimicrob Agents Chemother. 2001, 45(1): 229-235. 閵嗏偓閵嗏偓 [3] Bridges EG, et al. Nonclinical safety profile of telbivudine, a novel potent antiviral agent for treatment of hepatitis B. Antimicrob Agents Chemother. 2008, 52(7): 2521-2528. 閵嗏偓閵嗏偓 [4] Wu ZG, 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, 17 Suppl 1: 24-33. 閵嗏偓閵嗏偓 [5] Wu GY, et al. Inhibition of hepatitis B virus replication by Bay 41-4109 and its association with nucleocapsid disassembly. J Chemother. 2008, 20(4): 458-467. 閵嗏偓閵嗏偓

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