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[CAS NO. 106941-25-7]  Adefovir

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PRODUCTS SPECIFICATIONS [106941-25-7]

Catalog
HY-B1826
Brand
MCE
CAS
106941-25-7

DESCRIPTION [106941-25-7]

Overview

MDLMFCD00866943
Molecular Weight273.19
Molecular FormulaC8H12N5O4P
SMILESNC1=C2N=CN(CCOCP(O)(O)=O)C2=NC=N1

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE


Summary

Adefovir (GS-0393) is an adenosine monophosphate analog antiviral agent that after intracellular conversion to Adefovir diphosphate inhibits HBV DNA polymerase . Adefovir has an IC 50 of 0.7 μM against HBV in the HepG2.2.15 cell line. Adefovir has good antiviral activity against several viruses, including HBV and herpesviruses [1] [2] [3] .


IC50 & Target

HBV [1] [2] [3] ;
DNA polymerase [1] [2]


In Vitro

Studies to elucidate the mechanism of action of Adefovir against herpesvirus replication reveals that the phosphorylation of Adefovir occurred intracellularly and is carried out by host cellular enzymes. The diphosphorylated derivatives of Adefovir targeted the viral DNA polymerase and also acted as DNA chain terminators. Adenylate kinase is shown to be responsible for the first phosphorylation, which was followed by ADP kinase and creatine kinase, forming Adefovir diphosphate [1] .

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


In Vivo

Unaffected by food, Adefovir achieves 60% oral bioavailability. Its half-life is 12-30 hours and Adefovir undergoes renal excretion without significant metabolites. Adefovir does not substantially affect the cytochrome P450 system [3] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01300234 GlaxoSmithKline
Hepatitis B
March 30, 2011 Phase 3
NCT00986778 Bristol-Myers Squibb
Hepatitis B, Chronic
December 2009 Phase 4
NCT00002326 Gilead Sciences|NIH AIDS Clinical Trials Information Service
HIV Infections
Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

0.1 M NaOH : 10 mg/mL ( 36.60 mM ; ultrasonic and adjust pH to 10 with NaOH)

H 2 O : 1 mg/mL ( 3.66 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6605 mL 18.3023 mL 36.6046 mL
5 mM 0.7321 mL 3.6605 mL 7.3209 mL
10 mM 0.3660 mL 1.8302 mL 3.6605 mL
* Please refer to the solubility information to select the appropriate solvent.


Synonyms

Phosphonic acid, P-[[2-(6-amino-9H-purin-9-yl)ethoxy]methyl]-
Phosphonic acid, [[2-(6-amino-9H-purin-9-yl)ethoxy]methyl]-
P-[[2-(6-Amino-9H-purin-9-yl)ethoxy]methyl]phosphonic acid
9-(2-Phosphonylmethoxyethyl)adenine
PMEA
9-[2-(Phosphonomethoxy)ethyl]adenine
GS 0393
Adefovir
((2-(6-Amino-9H-purin-9-yl)ethoxy)methyl)phosphonicacid
[[2-(6-Amino-9H-purin-9-yl)ethoxy]methyl]phosphonic acid
2-(6-Aminopurin-9-yl)ethoxymethylphosphonic acid

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