1. Anti-infection
  2. HBV

Entecavir (Synonyms: BMS200475; SQ34676)

Cat. No.: HY-13623 Purity: 98.88%
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

Size Price Stock Quantity
10 mM * 1 mL in DMSO $139 In-stock
10 mg $126 In-stock
50 mg $189 In-stock
100 mg $338 In-stock
200 mg   Get quote  
500 mg   Get quote  

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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].

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].

Clinical Trial
Sponsor Condition Start Date Phase
Bristol-Myers Squibb Chronic Hepatitis B 2009-12-17 Phase 2
Bristol-Myers Squibb Chronic Hepatitis B 2011-09-16 Phase 2
References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
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].

References
M.Wt

277.28

Formula

C₁₂H₁₅N₅O₃

CAS No.

142217-69-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 44 mg/mL

Purity: 98.88%

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Product Name:
Entecavir
Cat. No.:
HY-13623
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