Entecavir monohydrate

SKU: orb1310955

Description

Entecavir monohydrate

Research Area

Infectious Disease & Virology

Key Properties

• CAS Number: 209216-23-9
• MW: 295.3
• Purity: 99.73%
• Formula: C₁₂H₁₅N₅O₃·H₂O
• SMILES: O.Nc1nc(=O)c2ncn([C@H]3C[C@H](O)[C@@H](CO)C3=C)c2[nH]1
• Target: HBV
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:55 mg/mL (186.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (8.47 mM)

Bioactivity

• Target IC50:
  HBV (HepG2 cells):3.75 nM(ec50)
• In Vivo:
  In liver biopsy Samples, Entecavir reduces both covalently closed circular DNA an the negativity o the hepatitis B virus core antigen. Entecavir triphosphate acts as an effective inhibitor o the wild-type HBV polymerase and is 100-300 times more potent than lamivudine triphosphate against 3TC-resistant HBV polymerase. To inhibi the replication of 3TC-resistant HBV, Entecavir requires a concentration that is 20-30 times higher. With an EC50 of 0.1 nM, Entecavir demonstrates significant activity against HIV. It can be utilized in a Single-cycle, Single-cell line pseudovirus assay, measuring green fluorescent protein in CD4+ lymphocytes using fluorescence-activated cell sorting.
• In Vitro:
  In ducks, Entecavir administration results in a 4-log reduction of serum DHBV DNA levels within 80 days and a 2- to 3-log decrease in hepatitis B virus surface antigen within 120 days. Treatment with Entecavir also decreases replication intermediates of DHBV DNA in the liver by a factor of 70, while covalently closed circular DNA levels are only reduced fourfold under stable template conditions. Additionally, Entecavir reduces bot the intensity of antigen staining an the percentage of antigen-positive cells in the liver, although there is an increase in antigen staining intensity in bile duct cells.
• 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 × 0^5 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 1.

Storage & Handling

• Storage: keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

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

Compound Identifiers

PubChem CID

135526609