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Purity: ≥98%
Pradefovir mesylate (formerly known as Remofovir mesylate, ICN-2001-3 mesylate, MB-06866 mesylate, MB-6866 mesylate, ICN-20013 mesylate) is an RTI (reverse transcriptase) inhibitor that has the potential for the treatment of chronic HBV infection. It is also a good substrate for liver CYP3A4. Pradefovir is prodrug of adefovir that is designed to target liver. Pradefovir can be activated to PMEA (9-(2-phosphonylmethoxyethyl)adenine ) in human liver microsomes with with a Km of 60 μM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 ml/min.
| ln Vitro |
Pradefovir is a PMEA prodrug that is cyclic diester. It is one of the HepDirect prodrugs made to be selectively and potently activated by oxidative processes mediated by the liver-based enzyme CYP3A4. With a Km of 60 μM, a maximum metabolic rate of 228 pmol/min/mg protein, and an intrinsic clearance rate of around 359 L/min, pradefovir is transformed into PMEA in human liver microsomes [1].
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| ln Vivo |
For eight days, rats were given 300 mg/kg of prdefovir orally. The rats' body weight, liver weight, liver weight to body weight ratio, liver microsomal protein content, total CYP content, enzyme levels of CYP1A, CYP2B, and CYP3A activity, and apoprotein content of CYP1A1, CYP2B1/2, CYP3A1/2, and CYP4A1/3 were all unaffected, suggesting that prdefovir does not induce CYP in rats [1].
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| References |
[1]. Lin CC, et al. Metabolic activation of Pradefovir by CYP3A4 and its potential as an inhibitor or inducer. Antimicrob Agents Chemother. 2006 Sep;50(9):2926-31
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| Molecular Formula |
C13H23CLN5O7PS
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| Molecular Weight |
519.90
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| CAS # |
625095-61-6
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| Related CAS # |
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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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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (192.34 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Ketoconazole inhibition of conversion of pradefovir to PMEA in human liver microsomes as a percentage of the control activity (mean;n= 2) versus the concentration of pradefovir.Antimicrob Agents Chemother.2006 Sep;50(9):2926-31. |
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Determination ofKi(slope versus [I] plot) for ketoconazole on conversion of pradefovir to PMEA (mean;n= 2).Antimicrob Agents Chemother.2006 Sep;50(9):2926-31. |
MAb 3A4 inhibition of conversion of pradefovir to PMEA (mean;n= 2) in human liver microsomes.Antimicrob Agents Chemother.2006 Sep;50(9):2926-31. |
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