| Description | Trifluoromethyl-tubercidin (TFMT) inhibits host MTr1 and suppresses virus replication. TFMT inhibits MTr1 through interaction at its S-adenosyl-l-methionine binding pocket to restrict influenza virus replication. TFMT was effective in inhibiting viral replication in mice, displayed little toxicity. |
| In vitro | Trifluoromethyl-tubercidin对IAV感染的中位抑制浓度（IC50）为0.30 μM，在有效浓度范围内未观察到明显的体外毒性，此通过水溶性四唑（WST）-8 细胞活力检测确定。Trifluoromethyl-tubercidin处理在感染后3至4小时显著抑制了IAV复制。在IAV感染的鼠细胞系LA-4中，Trifluoromethyl-tubercidin展示了抑制活性，尽管其效力（IC50 = 7.7 μM）低于在人类细胞中的效力[1]。 |
| In vivo | 在感染IAV后2天对小鼠进行Trifluoromethyl-tubercidin处理。此时，小鼠肺部的NP和PB2 mRNA水平因Trifluoromethyl-tubercidin处理而显著降低，表明Trifluoromethyl取代的tubercidin降低了体内毒性至我们无法检测的水平，但保持了抗IAV的功效[1]。 |
| molecular weight | 334.25 |
| Molecular formula | C12H13F3N4O4 |
| CAS | 1854086-05-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 3.34 mg/mL (10 mM) |
| References | 1. Tsukamoto Y, et al. Inhibition of cellular RNA methyltransferase abrogates influenza virus capping and replication. Science. 2023 Feb 10;379(6632):586-591. |