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Pradefovir

Catalog No. T28449 CAS 625095-60-5

Synonyms: ICN-2001-3, MB-6866, ICN-20013, MB-06866, Remofovir

Pradefovir (Remofovir) is a reverse transcriptase inhibitor potentially for treatment of chronic HBV infection. Pradefovir is also a liver-targeted prodrug of adefovir. After metabolic activation, Pradefovir was converted to PMEA (9-(2-phosphonylmethoxyethyl)adenine) in human liver microsomes with a K(m) of 60 microM, a maximum rate of metabolism of 228 pmol/min/mg protein, and an intrinsic clearance of about 359 ml/min.

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Pradefovir, CAS 625095-60-5

Pack Size	Availability	Price/USD	Quantity
25 mg	In stock	$ 1,300.00
50 mg	In stock	$ 1,690.00

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Purity: 97.50%

Biological Description

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Storage & Solubility Information

Description

In vivo

Pradefovir, a prodrug of PMEA, is under phase 2 clinical trial in China to evaluate its pharmacokinetic and pharmacodynamics after multiple-dose study, with adefovir dipivoxil and tenofovir disoproxil fumarate as positive control. A rapid and sensitive liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the quantification of pradefovir, PMEA and tenofovir in HBV patient serum. Serum samples were pretreated via simple protein precipitation with methanol and entecavir was used as internal standard. Chromatographic separation was carried out on a Synergi(?) fusion-RP column (150mm×4.6mm) by gradient elution with methanol and 0.1% formic acid in water (v/v) at a flow rate of 1mL/min. The analytes were detected in multiple reaction monitoring mode with positive ion electrospray ionization at m/z 424.1/151.0, 274.1/162.2, 288.1/176.1, and 278.1/152.2for pradefovir, PMEA, tenofovir and IS, respectively. The assays were validated according to current bioanalytical guidelines including specificity, linearity (2.0-500ng/mL for pradefovir and PMEA, 4.0-1000ng/mL for tenofovir), accuracy and precision, extraction recovery, matrix effect and stability. The validated method has been successfully applied to the pharmacokinetic study of pradefovir, adefovir dipivoxil and tenofovir disoproxil fumarate in a set of HBV patients[1].

Synonyms	ICN-2001-3, MB-6866, ICN-20013, MB-06866, Remofovir
Molecular Weight	423.79
Formula	C17H19ClN5O4P
CAS No.	625095-60-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Soluble

References and Literature

1. Xiao Q, Wang D, Yang W, Chen L, Ding Y, Yang J. Simultaneous determination of pradefovir, PMEA and tenofovir in HBV patient serum using liquid chromatography-tandem mass spectrometry and application to phase 2 clinical trial. J Chromatogr B Analyt Technol Biomed Life Sci. 2016 Jun 1;1022:133-40. doi: 10.1016/j.jchromb.2016.04.019. Epub 2016 Apr 11. PubMed PMID: 27089519. 2. Xiao Q, Yang W, Wang D, Chen L, Yuan L, Ding Y, Yang J. Factors limiting the extent of absolute bioavailability of pradefovir in rat. Xenobiotica. 2016 Oct;46(10):913-21. doi: 10.3109/00498254.2015.1133866. Epub 2016 Feb 5. PubMed PMID: 26846680. 3. Zhang Y, Shen L, Zhan Y, Xiao QQ, Yang J. Development and Validation of a Sensitive LC-MS-MS Method for the Determination of Adefovir in Human Serum and Urine: Application to a Clinical Pharmacokinetic Study. J Chromatogr Sci. 2016 Apr;54(4):507-15. doi: 10.1093/chromsci/bmv172. Epub 2015 Dec 10. PubMed PMID: 26657410; PubMed Central PMCID: PMC4885381. 4. Hynicka LM, Yunker N, Patel PH. A review of oral antiretroviral therapy for the treatment of chronic hepatitis B. Ann Pharmacother. 2010 Jul-Aug;44(7-8):1271-86. doi: 10.1345/aph.1M590. Epub 2010 Jun 29. Review. PubMed PMID: 20587747.

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Keywords

Pradefovir 625095-60-5 Microbiology/Virology HBV ICN 20013 MB 6866 ICN-2001-3 MB-6866 ICN20013 MB6866 MB 06866 ICN-20013 MB-06866 Remofovir MB06866 inhibitor inhibit

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