Cat. No. Name Size Price Add Cart
KI1026Entecavir hydrate50 mg$530
Entecavir hydrate100 mg$800

Chemical Characteristic

Product NameEntecavir hydrate
SynonymsBaraclude, ETV, Entaliv, BMS-200475
CAS No.209216-23-9
Molecular Weight 295.29
FormulaC12H17N5O4
Chemical Name2-amino-9-((1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-3H-purin-6(9H)-one hydrate
Smilesn1cn(c2nc([nH]c(=O)c12)N)C1C(=C)[C@@H]([C@H](C1)O)CO O
Chemical Structure

Biological activities

Entecavir is a potent and selective inhibitor of hepatitis B virus. Entecavir is used in the treatment of hepatitis B infection. The IC50 of entecavir is 3 nM against hepatitis B virus. Entecavir has relatively low cytotoxicity with a CC50 ranging from 21 to 120 µM.[1] In addition, the IC50 of entecavir is 3.75 nM against HepG2 stably transfected cell line 2.2.15 with hepatitis B virus.[2] Entecavir inhibits DHBV-infected duck hepatocytes with an IC50 of 0.13 nM. In contrast, entecavir prevents 3TC cells with an IC50 of 138 nM. Reducing the daily dose of entecavir to only 0.01 mg/kg results in an average viral DNA level decrease of log10 0.97. [3]

References

[1] Bisacchi GS, et al.BMS-200475, a novel carbocyclic 2??deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro. Bioorganic & Medicinal Chemistry Letters. 1997, 7(2): 127-132.
[2] Innaimo SF, et al. Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother. 1997, 41(7): 1444-1448.
[3] Marion PL, et al. Potent efficacy of entecavir (BMS-200475) in a duck model of hepatitis B virus replication. Antimicrob Agents Chemother. 2002, 46(1): 82-88.

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