Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Adefovir (formerly known as PMEA and GS-0393; trade names Preveon and Hepsera) is a potent DNA polymerase inhibitor with the potential for the treatment of HBV infection.
ln Vitro |
Adefovir diphosphate functions as a DNA terminator in addition to targeting viral DNA polymerase. The first phosphorylation was found to be caused by adenylate oxidation, which was then followed by the oxidation of creatine and ADP to produce adefovir diphosphate [1].
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ln Vivo |
Adefovir diaphragm has a 60% bioavailability and is not impacted by food. It has a 12-to 30-hour half-life. Adefovir has no discernible metabolites and is eliminated by the kidneys. In general, adefovir has no effect on cytochrome P450[3].
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References |
[1]. X.-X.Zhou, et al. 7.11 - Deoxyribonucleic Acid Viruses: Antivirals for Herpesviruses and Hepatitis B Virus. Comprehensive Medicinal Chemistry II. Volume 7, 2007, Pages 295-327.
[2]. Marcellin P, et al. Adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B. N Engl J Med. 2003 Feb 27;348(9):808-16. [3]. Leah A.Burke, et al. 155 - Drugs to Treat Viral Hepatitis. Infectious Diseases. Volume 2, 2017, Pages 1327-1332. |
Molecular Formula |
C8H12N5O4P
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Molecular Weight |
273.18
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Exact Mass |
273.0627
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CAS # |
106941-25-7
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Related CAS # |
Adefovir-d4;1190021-70-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
NC1=C2N=CN(CCOCP(O)(O)=O)C2=NC=N1
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InChi Key |
SUPKOOSCJHTBAH-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C8H12N5O4P/c9-7-6-8(11-3-10-7)13(4-12-6)1-2-17-5-18(14,15)16/h3-4H,1-2,5H2,(H2,9,10,11)(H2,14,15,16)
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Chemical Name |
((2-(6-amino-9H-purin-9-yl)ethoxy)methyl)phosphonic acid
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Synonyms |
GS-0393 GS-393 GS0393 GS393 GS 0393 GS 393 PMEA
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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) |
0.1 M NaOH : ~10 mg/mL (~36.60 mM)
H2O : ~1 mg/mL (~3.66 mM) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6606 mL | 18.3030 mL | 36.6059 mL | |
5 mM | 0.7321 mL | 3.6606 mL | 7.3212 mL | |
10 mM | 0.3661 mL | 1.8303 mL | 3.6606 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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01546116 | Completed | Drug: ADEFOVIR, LAMIVUDINE | Chronic Hepatitis B | Korea University | February 2010 | Phase 4 |
NCT01329419 | Completed Has Results | Drug: adefovir dipivoxil | Hepatitis B | GlaxoSmithKline | August 2004 | |
NCT00187746 | Withdrawn | Drug: Adefovir dipivoxil | Other Conditions That May Be A Focus of Clinical Attention |
University of California, San Francisco | August 2005 | Phase 4 |
NCT00441974 | Completed Has Results | Drug: adefovir dipivoxil | Chronic Hepatitis B | GlaxoSmithKline | December 2006 | Phase 4 |
Mean Change from Base Line in Serum Levels of Hepatitis B Virus (HBV) DNA. td> |