Foscarnet sodium (Phosphonoformate) is an antiviral agent used in the treatment of cytomegalovirus retinitis. Foscarnet also shows activity against human herpesviruses and HIV.

Foscarnet Sodium能夠穿透細胞膜，通过抑制病毒DNA合成来抑制病毒复制。在感染了HTLV-III的H9细胞中，Foscarnet Sodium (300 μM) 对HTLV-III逆转录酶活性的抑制率超過95%。[1] Foscarnet Sodium的细胞毒性较低，但在高浓度下可抑制细胞增殖，此效应可通过去除化合物逆转。与HeLa细胞或原代人肺成纤维细胞共同培养0.5-1 mM Foscarnet Sodium 24-48小时可抑制50%的DNA合成和/或细胞增殖。[1] Foscarnet Sodium能结合FGF2的肝素结合域，从而抑制FGF2诱导的细胞增殖。Foscarnet Sodium (25 μM) 处理HUVEC细胞48小时可减少FGF2诱导的细胞增殖20%。Foscarnet Sodium (0.5-1 mM) 将表达FGF2的人甲状腺未分化癌细胞系CAL-62的24小时增殖率降至约80%。[2]

Foscarnet Sodium 对感染病毒的动物，如皮肤感染、疱疹性角膜炎、生殖器感染、全身感染和脑间感染等，具有高效的治疗效果。例如，在接种后 48 小时开始使用Foscarnet Sodium（100 毫摩尔），每天使用两次，每次 30 微升，连续使用 4 天，可使 HSV-1 株 C42 接种后的累积评分降低 70% 以上。用 Foscarnet Sodium（20 mg/kg）作为气雾剂给感染小鼠 CMV 的小鼠注射，可使肺部滴度降低 60%。[1]

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.

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.(Only for Reference)