Formulation: A solid
Formal Name: 2-amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one
Purity: ≥99% deuterated forms (d1-d2)
Formula Markup: C12H13D2N5O3
Formula Weight: 279,3
Shelf life (days): 1460
Notes: Entecavir-d2 is intended for use as an internal standard for the quantification of entecavir (Item Nos. 36926 / 13831) by GC- or LC-MS. Entecavir is an antiviral nucleoside analog of 2'-deoxyguanosine (Item No. 9002864) and inhibitor of hepatitis B virus (HBV) reverse transcriptase (IC50 = 0.5 nM).{22164,59703} It undergoes phosphorylation by cellular kinases to its active form, entecavir triphosphate.{59703,53861} Entecavir reduces virion DNA in the culture supernatant of HepG2 2.2.15 cells infected with hepatitis B virus (HBV; EC50 = 3.75 nM).{22164} It reduces serum and hepatic levels of viral DNA in a duckling model of HBV infection when administered at a dose of 1 mg/kg.{22166} Formulations containing entecavir have been used in the treatment of chronic HBV infection.
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