1. Metabolic Enzyme/Protease
  2. Cytochrome P450

Pradefovir mesylate (Synonyms: Remofovir mesylate)

Cat. No.: HY-112690A Purity: 99.83%
Handling Instructions

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

For research use only. We do not sell to patients.

Pradefovir mesylate Chemical Structure

Pradefovir mesylate Chemical Structure

CAS No. : 625095-61-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 629 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a Km of 60 μM.

In Vitro

Pradefovir is a cyclodiester prodrug of PMEA. It is one of the HepDirect prodrugs, which are designed to be efficiently and specifically activated through an oxidative reaction catalyzed by CYP3A4, which is located mainly in the liver. Pradefovir is converted to PMEA in human liver microsomes with a Km of 60 μM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 L/min[1].

In Vivo

Daily oral dosing of Pradefovir (300 mg/kg) to rats for 8 days does not affect body weight; liver weight; liver weight-body weight ratio; liver microsomal protein content; total CYP content; enzyme activities for CYP1A, CYP2B, and CYP3A; and apoprotein contents for CYP1A1, CYP2B1/2, CYP3A1/2, and CYP4A1/3, indicating that Pradefovir is not a CYP inducer in rats[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

H2O : ≥ 125 mg/mL (240.43 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9234 mL 9.6172 mL 19.2345 mL
5 mM 0.3847 mL 1.9234 mL 3.8469 mL
10 mM 0.1923 mL 0.9617 mL 1.9234 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats[1]
Five rats receive Pradefovir (300 mg/kg/day) orally for 8 days. At 24 h after administration of the last dose, the rats are killed and liver samples are collected. Body weight, liver weight, liver protein content, and liver microsomal P450 contents are determined. The apoprotein levels for CYP1A1, CYP2B1/2B2, CYP3A1/3A2, and CYP4A1/4A3 and the enzyme activities for CYP1A, CYP2B, and CYP3A are also determined by Western blot and LC analysis, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

519.90

Formula

C₁₈H₂₃ClN₅O₇PS

CAS No.

625095-61-6

SMILES

NC1=C2N=CN(CCOC[[email protected]]3(OCC[[email protected]@H](C4=CC=CC(Cl)=C4)O3)=O)C2=NC=N1.CS(=O)(O)=O

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

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Product Name:
Pradefovir mesylate
Cat. No.:
HY-112690A
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Pradefovir mesylate

Cat. No.: HY-112690A