1. Anti-infection
  2. HBV
  3. Entecavir

Entecavir (Synonyms: BMS200475; SQ34676)

Cat. No.: HY-13623
Handling Instructions

Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.

For research use only. We do not sell to patients.

Entecavir Chemical Structure

Entecavir Chemical Structure

CAS No. : 142217-69-4

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Description

Entecavir (SQ 34676; BMS 200475) is a potent and selective inhibitor of HBV, with an EC50 of 3.75 nM in HepG2 cell.

IC50 & Target

EC50: 3.75 nM (anti-HBV, HepG2 cell)[2]

In Vitro

BMS-200475 has a EC50 of 3.75 nM against HBV. It is incorporated into the protein primer of HBV and subsequently inhibits the priming step of the reverse transcriptase. The antiviral activity of BMS-200475 is significantly less against the other RNA and DNA viruses[1]. Entecavir is more readily phosphorylated to its active metabolites than other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine. The intracellular half-life of entecavir is 15 h[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Daily oral treatment with BMS-200475 at doses ranging from 0.02 to 0.5 mg/kg of body weight for 1 to 3 months effectively reduces the level of woodchuck hepatitis virus (WHV) viremia in chronically infected woodchucks[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

277.28

Formula

C₁₂H₁₅N₅O₃

CAS No.
SMILES

O=C1NC(N)=NC2=C1N=CN2[[email protected]@H]3C([[email protected]](CO)[[email protected]@H](O)C3)=C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (158.68 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6065 mL 18.0323 mL 36.0646 mL
5 mM 0.7213 mL 3.6065 mL 7.2129 mL
10 mM 0.3606 mL 1.8032 mL 3.6065 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

BMS 200475 is prepared in phosphate-buffered saline (PBS) and diluted with appropriate medium containing 2% fetal bovine serum. HepG2 2.2.15 cells are plated at a density of 5×105 cells per well on 12-well Biocoat collagen-coated plates and are maintained in a confluent state for 2 to 3 days before being overlaid with 1 mL of medium spiked with BMS 200475. Quantification of HBV was performed on day 10[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

EntecavirBMS200475 SQ34676BMS 200475BMS-200475SQ34676SQ 34676SQ-34676HBVHepatitis B virusInhibitorinhibitorinhibit

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Entecavir
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