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Pradefovir mesylate

Catalog No. T19526Cas No. 625095-61-6
Alias Remofovir mesylate, Pradefovir mesilate, Hepavir B

Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.

Pradefovir mesylate

Pradefovir mesylate

Purity: 98%
Catalog No. T19526Alias Remofovir mesylate, Pradefovir mesilate, Hepavir BCas No. 625095-61-6
Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.
Pack SizePriceAvailabilityQuantity
1 mg$139In Stock
5 mg$349In Stock
10 mg$562In Stock
25 mg$889In Stock
50 mg$1,190In Stock
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Purity:98%
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Product Introduction

Bioactivity
Description
Pradefovir mesylate (Hepavir B) is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with Km of 60 μM.
Targets&IC50
CYP3A4:60 μM(Km,liver)
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 inhibits the conversion of pradefovir to PMEA in human liver microsomes, suggesting 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.
In vivo
In rats, the liver was the site of metabolic activation of pradefovir, whereas the small 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 rats[1].?
AliasRemofovir mesylate, Pradefovir mesilate, Hepavir B
Chemical Properties
Molecular Weight519.9
FormulaC18H23ClN5O7PS
Cas No.625095-61-6
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 120 mg/mL (230.81 mM)
Solution Preparation Table
H2O
1mg5mg10mg50mg
1 mM1.9234 mL9.6172 mL19.2345 mL96.1723 mL
5 mM0.3847 mL1.9234 mL3.8469 mL19.2345 mL
10 mM0.1923 mL0.9617 mL1.9234 mL9.6172 mL
20 mM0.0962 mL0.4809 mL0.9617 mL4.8086 mL
50 mM0.0385 mL0.1923 mL0.3847 mL1.9234 mL
100 mM0.0192 mL0.0962 mL0.1923 mL0.9617 mL

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