Viral polymerase-IN-1 hydrochloride

Viral polymerase-IN-1 hydrochloride, a Gemcitabine (HY-17026) derivative, potently inhibits influenza A and B viruses infection with IC90 values of 11.4-15.9 μM. Viral polymerase-IN-1 hydrochloride is active against SARS-CoV-2 infection. Viral polymerase-IN-1 hydrochloride suppresses influenza virus infection by affecting viral RNA replication/transcription in cells[1].

Signaling Pathways >> Anti-infection >> Influenza Virus

Research Areas >> Infection

Signaling Pathways >> Anti-infection >> SARS-CoV

IC50: 6.4 μM (H1N1) and 5.0 μM (H1N1)[1]

Viral polymerase-IN-1 hydrochloride (化合物 2h; 0.1, 1, 10 μM; 过夜) 以剂量依赖性方式降低病毒 NP 蛋白表达和病毒 RNA 拷贝[1]。 Viral polymerase-IN-1 hydrochloride (11, 33, 100 μM; 72 小时) 以剂量依赖的方式有效抑制病毒聚合酶活性，从而抑制人细胞 HeLa 中甲型流感病毒 PR8 的聚合酶活性[1]。 Viral polymerase-IN-1 hydrochloride 有效抑制 SARS-CoV-2 感染，在 Calu-3 细胞中 EC50 值为 0.46 μM，CC50 值高于 100 μM，SI 值>217.4[1]。 Western Blot Analysis[1] Cell Line: MDCK cells infected PR8 virus Concentration: 0.1, 1, 10 μM Incubation Time: Overnight Result: Reduced viral NP protein expression and viral RNA copies in a dose-dependent manner.

Viral polymerase-IN-1 hydrochloride (化合物 2h; 5 mg/kg; 腹腔给药; 每天一次; 持续 5 天; 在病毒感染前 4 小时开始) 不仅可以降低小鼠肺部的病毒 RNA 水平，还可以减轻感染介导的肺部浸润[1]。 Animal Model: Six-week-old BALB/c female mice intranasal infection with maPR8[1] Dosage: 5 mg/kg Administration: IP; once daily for 5 days, beginning 4 h prior to virus infection Result: Alleviated lung damage or reduced viral RNA replication.

[1]. Hyeon-Min Cha, et al. Evaluation of Antiviral Activity of Gemcitabine Derivatives against Influenza Virus and Severe Acute Respiratory Syndrome Coronavirus 2. ACS Infect Dis. 2023 Apr 14;9(4):1033-1045.