product name Entecavir Hydrate
Description: Entecavir, a new deoxyguanine nucleoside analogue, is a reverse transcriptase inhibitor. It is an oral antiviral drug used in the treatment of hepatitis B virus (HBV) infection. It prevents the hepatitis B virus from multiplying and reduces the amount of virus in the body. Entecavir is a highly potent inhibitor of wild-type HBV Pol and is 100- to 300-fold more potent than lamivudine-triphosphate against 3TC-resistant HBV Pol. Entecavir inhibits the replication of 3TC-resistant HBV, but 20- to 30-fold higher concentrations are required.
References: Antimicrob Agents Chemother. 2002 Aug;46(8):2525-32; Antimicrob Agents Chemother. 2003 Aug;47(8):2624-35.
295.29
Formula
C12H15N5O3.H2O
CAS No.
209216-23-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 59 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Entecavir-triphosphate is a highly potent inhibitor of wild-type HBV Pol and is 100- to 300-fold more potent than lamivudine-triphosphate against 3TC-resistant HBV Pol. Entecavir inhibits the replication of 3TC-resistant HBV, but 20- to 30-fold higher concentrations are required. Entecavir results in an impressive reduction of serum viral DNA with covalently closed circular DNA and hepatitis B viral core antigen negativity in liver biopsy specimens. Entecavir has potent activity (EC50, 0.1 nM) against HIV in a unique single-cycle, single-cell-based pseudovirus assay (24) with CD4+ lymphocytes using a green fluorescent protein reporter fluorescence-activated cell sorter assay as the endpoint. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Entecavir causes a 4-log drop in serum DHBV DNA levels within 80 days and a slower 2- to 3-log drop in serum DHBV surface antigen (DHBsAg) levels within 120 days in ducks. Entecavir treatment reduces DHBV DNA replicative intermediates 70-fold in the liver, while the level of the stable, template form, covalently closed circular DNA decreases only 4-fold in ducks. Entecavir treatment reduces both the intensity of antigen staining and the percentage of antigen-positive hepatocytes in the liver, but the intensity of antigen staining in bile duct cells appeares not to be effected in ducks. |
| Animal model | |
| Formulation & Dosage | |
| References | Antimicrob Agents Chemother. 2002 Aug;46(8):2525-32; Antimicrob Agents Chemother. 2003 Aug;47(8):2624-35. |
