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Foscarnet Sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Foscarnet Sodium图片
CAS NO:63585-09-1
规格:≥98%
包装与价格:
包装价格(元)
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
10g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)191.95
FormulaCNa3O5P
CAS No.63585-09-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 7 mg/mL (36.5 mM)
Water: 3 mg/mL (15.6 mM)
Ethanol: <1 mg/mL
Other info

Chemical Name: trisodium;phosphonatoformate

InChi Key: DFHAXXVZCFXGOQ-UHFFFAOYSA-K

InChi Code: InChI=1S/CH3O5P.3Na/c2-1(3)7(4,5)6;;;/h(H,2,3)(H2,4,5,6);;;/q;3*+1/p-3

SMILES Code: C(=O)([O-])P(=O)([O-])[O-].[Na+].[Na+].[Na+]

SynonymsPhosphonoformate; Trisodium phosphonoformate; Phosphonoformic acid trisodium salt
实验参考方法
In Vitro

In vitro activity: Foscarnet Sodium is able to penetrate into cells and inhibit viral replication by inhibiting viral DNA synthesis. Foscarnet Sodium (300 μM) displays a more than 95% inhibition on HTLV-III reverse transcriptase activity in H9 cells infected with HTLV-III. Foscarnet Sodium 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 Foscarnet Sodium with HeLa cells or primary human lung fibroblast for 24-48 hr inhibited 50% DNA synthesis and/or cell proliferation. Foscarnet Sodium is able to bind with the heparin-binding domain of FGF2 and inhibits FGF2 induced cell proliferation. Foscarnet Sodium (25 μM) treating HUVEC cells for 48 hr reduced FGF2-induced cellular proliferation by 20%. Foscarnet Sodium (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%.


Kinase Assay: 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.


Cell Assay: CAL-62 cells are placed on 96 well plates at 8×103 cells/well in 100 μL DMEM for 24 h. Then medium is replaced by fresh DMEM with or without foscarnet. After 48 h of incubation, 20 μL of CellTiter 96AQ solution is added to the cells and incubated for 2-4 h. The quantity of formazan product as measured by the absorbance at 492 nm.

In VivoFoscarnet 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, Foscarnet Sodium (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. Foscarnet Sodium (20 mg/kg) given as an aerosol to mice infected with murine CMV caused a reduction of 60% in lung titers.
Animal modelGuinea-pigs with cutaneous HSV-1 infections on the backs
Formulation & DosageDissolved in Water solution with 0.1% Tween 80 and 10% (wt/wt) glycerol and adjusted to pH 6.0; 5 mM; Topical application
References

Pharmacol Ther. 1989;40(2):213-85; Biomed Pharmacother. 2013 Feb;67(1):53-7.