Entecavir Monohydrate
-
- Category :
Pharmaceuticals and Biochemicals
- CAS NO : 209216-23-9
- EC NO :
- Molecular Formula : C12H17N5O4
- Main Specifications : Up to Merck Standard
- Synonyms : 2-Amino-1,9-dihydro-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one monohydrate;2-amino-9-[(3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-3,9-dihydro-6H-purin-6-one hydrate (1:1);Entecavir Monohydrate;Enticavir hydrate;
Package: 25kgs net per fiber drum
Molecular Structure:
Product description:
Entecavir monohydrate is a guanosine nucleoside analogue with activity against HBV polymerase. It is phosphorylated to the active triphosphate (TP) form, which has an intracellular half-life of 15 hours. Intracellular TP levels are directly related to extracellular entecavir monohydrate concentrations, with no significant accumulation beyond initial plateau levels. By competing with the natural substrate deoxyguanosine-TP, entecavir monohydrate-TP inhibits all 3 functional activities of the viral polymerase: (1) priming of the HBV polymerase, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA. Entecavir monohydrate-TP Ki value for inhibition of HBV DNA polymerase is 1.2 nM. Entecavir monohydrate-TP is a weak inhibitor of cellular DNA polymerases α, ?, δand εwith Ki values of 18 to 40 μM. It did not inhibit mitochondrial γ polymerase (Ki>160μM) and did not affect the mitochondrial DNA content of human hepatoma cells in vitro. Entecavir monohydrate inhibited HBV DNA synthesis at a concentration of 0.004μM in human HepG2 cells transfected with wild-type HBV. IC50 values for entecavir monohydrate against lamivudine-resistant HBV ranged from 0.029-0.061 μM.
If you are sourcing Entecavir Monohydrate from China ,just feel free to inquire
Search Product