1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Pradefovir mesylate

Pradefovir mesylate  (Synonyms: Remofovir mesylate)

Cat. No.: HY-112690A Purity: 99.53%
COA 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

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Solution
10 mM * 1 mL in Water USD 629 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
1 mg USD 261 In-stock
5 mg USD 550 In-stock
10 mg USD 850 In-stock
25 mg USD 1700 In-stock
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Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Pradefovir mesylate

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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.

IC50 & Target

CYP3

 

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].

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

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].

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

Clinical Trial
Molecular Weight

519.90

Appearance

Solid

Formula

C18H23ClN5O7PS

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (192.34 mM; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (192.34 mM); Clear solution; Need ultrasonic

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.89%

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
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Pradefovir mesylate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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