[CAS NO. 625095-61-6] Pradefovirmesylate
PRODUCTS SPECIFICATIONS [625095-61-6]
DESCRIPTION [625095-61-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 519.90 |
| Molecular Formula | C18H23ClN5O7PS |
| SMILES | NC1=C2N=CN(CCOC[P@]3(OCC[C@@H](C4=CC=CC(Cl)=C4)O3)=O)C2=NC=N1.CS(=O)(O)=O |
1 Publications Citing Use of MCE
Summary
Pradefovir mesylate is a good substrate for liver CYP3A4. Pradefovir is converted to 9-(2-phosphonylmethoxyethyl)adenine (PMEA) in human liver microsomes with a K m 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 K m 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
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04543565 | Xi´an Xintong Pharmaceutical Research Co.,Ltd. |
Chronic Hepatitis b
|
September 2020 | Phase 3 |
| NCT00230503 | Bausch Health Americas, Inc. |
Hepatitis B, Chronic
|
June 2004 | Phase 2 |
| NCT00230490 | Bausch Health Americas, Inc. |
Hepatitis B, Chronic
|
June 2005 | Phase 2 |
Appearance
Solid
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
H 2 O : 100 mg/mL ( 192.34 mM ; Need ultrasonic)
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 |
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1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (192.34 mM); Clear solution; Need ultrasonic
Synonyms
