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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in Water
ready for reconstitution
USD 629 In-stock
Solution
10 mM * 1 mL in Water USD 629 In-stock
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
50 mg   Get quote  
100 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Pradefovir mesylate

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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].

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

Clinical Trial
Molecular Weight

519.90

Formula

C18H23ClN5O7PS

CAS No.
Appearance

Solid

Color

White to off-white

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

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

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 1.9234 mL 9.6172 mL 19.2345 mL 48.0862 mL
5 mM 0.3847 mL 1.9234 mL 3.8469 mL 9.6172 mL
10 mM 0.1923 mL 0.9617 mL 1.9234 mL 4.8086 mL
15 mM 0.1282 mL 0.6411 mL 1.2823 mL 3.2057 mL
20 mM 0.0962 mL 0.4809 mL 0.9617 mL 2.4043 mL
25 mM 0.0769 mL 0.3847 mL 0.7694 mL 1.9234 mL
30 mM 0.0641 mL 0.3206 mL 0.6411 mL 1.6029 mL
40 mM 0.0481 mL 0.2404 mL 0.4809 mL 1.2022 mL
50 mM 0.0385 mL 0.1923 mL 0.3847 mL 0.9617 mL
60 mM 0.0321 mL 0.1603 mL 0.3206 mL 0.8014 mL
80 mM 0.0240 mL 0.1202 mL 0.2404 mL 0.6011 mL
100 mM 0.0192 mL 0.0962 mL 0.1923 mL 0.4809 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Pradefovir mesylate
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