Pradefovir mesylate

SKU: orb1306990

Description

Pradefovir mesylate

Research Area

Metabolism Research

Key Properties

• CAS Number: 625095-61-6
• MW: 519.9
• Purity: 98.00%
• Formula: C₁₈H₂₃ClN₅O₇PS
• SMILES: CS(O)(=O)=O.Nc1c2ncn(CCOC[P@@](OCC3)(O[C@@H]3c3cccc(Cl)c3)=O)c2ncn1
• Target: Cytochromes P450
• Solubility: H2O:120 mg/mL (230.81 mM)

Bioactivity

• Target IC50:
  CYP3A4:60 μM(Km,liver)
• In Vivo:
  In rats the liver wa the site of metabolic activation of pradefovir, wherea the s All intestine did not play a significant role in the metabolic conversion of pradefovir to PMEA. Daily oral dosing (300 mg/kg) to rats for 8 days showed that pradefovir was not an inducer of P450 enzymes in rat.
• In Vitro:
  Pradefovir was converted to PMEA in human liver microsomes with a K(m) of 60 microM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 ml/min. Addition of ketoconazole and monoclonal antibody 3A4 significantly inhibit the conversion of pradefovir to PMEA in human liver microsomes, suggestin the predominant role of CYP3A4 in the metabolic activation of pradefovir. Pradefovir at 0.2, 2, and 20 microM was neither a Direct inhibitor nor a mechanism-based inhibitor of CYP3A4, CYP2D6, CYP2C9, CYP2C19, CYP2E1, and CYP1A2 in human liver microsomes.

Storage & Handling

• Storage: 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

CYP3A4, CYPs, Cytochrome P450, Inhibitor, Hepavir B, inhibit, Remofovir, Remofovir Mesylate, Remofovir mesylate, Pradefovir, Pradefovir mesilate, Pradefovir mesylate, Pradefovir Mesylate

Compound Identifiers

PubChem CID

9604653