Pradefovir mesylate
Based on 1 publication(s) in Google Scholar
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.
- Purity: 99.53%
- CAS No.: 625095-61-6
- Formula: C18H23ClN5O7PS
- Molecular Weight:519.90
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Pradefovir mesylate
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Biological Activity
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CYP3 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 625095-61-6
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Appearance Solid
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Molecular Weight 519.90
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Formula C18H23ClN5O7PS
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Color White to off-white
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SMILES
NC1=C2N=CN(CCOC[P@]3(OCC[C@@H](C4=CC=CC(Cl)=C4)O3)=O)C2=NC=N1.CS(=O)(O)=O
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Synonyms
Remofovir mesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Pharm
2018 Dec 3;15(12):5646-5652. PMID: 30375875
Solvent & Solubility
H2O : 100 mg/mL (192.34 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (192.34 mM); Clear solution; Need ultrasonic
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
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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