Entecavir

SKU: orb1310954

Description

Entecavir (SQ34676) is a guanosine nucleoside analogue used to treat chronic hepatitis B virus (HBV) infection. It is widely applied in antiviral research, with established in vitro and in vivo models for studying HBV replication and therapy-associated hepatitis flares.

Research Area

Infectious Disease & Virology

Key Properties

• CAS Number: 142217-69-4
• MW: 277.28
• Purity: 99.72%
• Formula: C₁₂H₁₅N₅O₃
• SMILES: Nc1nc2n(cnc2c(=O)[nH]1)[C@H]1C[C@H](O)[C@@H](CO)C1=C
• Target: HBV
• Solubility: DMSO:63.13 mg/mL (227.68 mM);5% DMSO+95% Saline:1 mg/mL (3.61 mM)

Bioactivity

• Target IC50:
  HBV (HepG2 cells):3.75 nM(ec50)
• In Vivo:
  Administering BMS-200475 orally on a daily basis in doses between 0.02 and 0.5 mg/kg of body weight for a duration of one to three months significantly decreases the viremia level of woodchuck hepatitis virus (WHV) in chronically infected woodchucks.
• In Vitro:
  BMS-200475 demonstrates potent antiviral activity with an EC50 of 3.75 nM against HBV by integrating into the protein primer of HBV, thereby inhibiting the priming step of the virus's reverse transcriptase. Its efficacy is notably reduced against other RNA and DNA viruses. Entecavir, compared to other deoxyguanosine analogs (penciclovir, ganciclovir, lobucavir, and aciclovir) or lamivudine, undergoes more efficient phosphorylation to its active metabolites. Additionally, entecavir has an intracellular half-life of 15 hours.
• Cell Research:
  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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Entecavir, Inhibitor, Hepatitis B virus, HBV( HepG2 cell), HBV, inhibit, BMS 200475, BMS200475, BMS-200475, SQ 34676, SQ34676, SQ-34676

Compound Identifiers

PubChem CID

135398508