| Description | BMY-27709 is an influenza virus growth inhibitor with an IC50 value of 3-8 μM against A/WSN/33 virus growth, and also exhibits inhibitory activity against some subtypes of influenza viruses.BMY-27709 acts early in the course of H1 and H2 virus infections, and exhibits antiviral activity through inhibition of hemagglutinin proteins. However, BMY-27709 has no effect on H3 subtype viruses and influenza B/Lee/40 viruses. |
| In vitro | BMY-27709对WSN 33病毒的多周期复制实验中具有3-8μM的IC50值，可有效抑制所有经测试的H1和H2亚型病毒。然而，BMY-27709对H3亚型病毒和流感B/Lee/40病毒无活性。研究发现，BMY-27709能在感染初期对H1和H2病毒发挥作用，暗示其抑制靶点为血凝素蛋白。通过使用重排病毒和分离对BMY-27709具有抗性的病毒得到了证实。分离出的抗性病毒在HA2亚单位的第110个氨基酸位置由苯丙氨酸变为丝氨酸。通过逆向遗传学证明了这一单一突变是导致获得对BMY-27709抗性的原因，即仅包含此变化的转染病毒表现出对BMY-27709的抗性，而无此突变的对照病毒则仍然敏感。BMY-27709能够抑制病毒引发的红细胞溶血，表明它阻断了血凝素的膜融合功能。这些实验进一步说明流感病毒的血凝素蛋白是发现和开发小分子病毒生长抑制剂的有效靶标。 |
| Synonyms | BMY 27709, BMY27709 |
| molecular weight | 337.84 |
| Molecular formula | C17H24ClN3O2 |
| CAS | 99390-76-8 |
| Storage | |Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 50 mg/mL (148 mM) |
| References | 1. Luo G, et al. Characterization of a hemagglutinin-specific inhibitor of influenza A virus. Virology. 1996;226(1):66-76. 2. Luo G, et al. Molecular mechanism underlying the action of a novel fusion inhibitor of influenza A virus. J Virol. 1997;71(5):4062-4070. 3. Combrink KD, et al. Salicylamide inhibitors of influenza virus fusion. Bioorg Med Chem Lett. 2000;10(15):1649-1652. 4. Hsieh HP, et al. Strategies of development of antiviral agents directed against influenza virus replication. Curr Pharm Des. 2007;13(34):3531-3542. |