Home Microbiology Reverse Transcriptase inhibitor Foscarnet Sodium

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Foscarnet Sodium Reverse Transcriptase inhibitor

Cat.No.S3076

Foscarnet Sodium (Phosphonoformate) inhibits viral RNA polymerases, reverse transcriptase, and DNA polymerases through noncompetitive inhibition with dNTPs.
Foscarnet Sodium Reverse Transcriptase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 191.95

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Chemical Information, Storage & Stability

Molecular Weight 191.95 Formula

CNa3O5P

 Storage (From the date of receipt)
CAS No. 63585-09-1 Download SDF Storage of Stock Solutions

Synonyms Phosphonoformate Smiles C(=O)([O-])P(=O)([O-])[O-].[Na+].[Na+].[Na+]

Solubility

In vitro
Batch:

Water : 19 mg/mL

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
RNA polymerase [1]
reverse transcriptase [1]
DNA polymerase [1]
In vitro
Foscarnet Sodium is able to penetrate into cells and inhibit viral replication by inhibiting viral DNA synthesis. This compound (300 μM) displays a more than 95% inhibition on HTLV-III reverse transcriptase activity in H9 cells infected with HTLV-III. [1] It has a low cellular toxicity, but shows an inhibition of cell proliferation at high concentrations, which is reversed after drug removal. Incubation 0.5-1 mM of this chemical with HeLa cells or primary human lung fibroblast for 24-48 hr inhibited 50% DNA synthesis and/or cell proliferation. [1] This compound is able to bind with the heparin-binding domain of FGF2 and inhibits FGF2 induced cell proliferation. It (25 μM) treating HUVEC cells for 48 hr reduced FGF2-induced cellular proliferation by 20%. This chemical (0.5-1 mM) reduced the 24h proliferation rate of CAL-62 cell, a Human thyroid anaplastic carcinoma cell line which expresses FGF2, to nearly 80%. [2]
Kinase Assay
Reverse transcriptase assays
Reverse transcriptase assays are carried out in a reaction mixture (50 μL) containing 50 mM Tris-HCl (pH 7.5), 5 mM DTT, 100 mM potassium chloride, 0.01% Triton X-100 or NP40, 10 μg/ml (dT)15.(A)n as template primer and [3H] deoxythymidine triphospahate. The reaction mixture is incubated for 1 hr at 37 ℃ and stopped by the addition of 50 μg of yeast tRNA and 2 mL of 10% solution of trichloroacetic acid containing 1 mM sodium pyrophosphate. The samples are filtered on filters (0.45 μm), washed first with 5% TCA solution for 5 times and then with 2 ml of 70% ethanol. The filters are dried, scintillation fluid is added and the radioactivity counted in a counter.
In vivo
Foscarnet Sodium display an efficient therapy effect on animal with virus diseases, such as cutaneous infection, herpes keratitis, genital infection, or systemic and interacerebral infection. For example, this compound (100 mM) applied at initiated 48 h post inoculation with twice daily applications of 30 μL for 4 days, displays a more than 70% reduction in cumulative score after inoculation with HSV-1 strain C42. This chemical (20 mg/kg) given as an aerosol to mice infected with murine CMV caused a reduction of 60% in lung titers. [1]
References

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