产品
编 号:F761702
分子式:C29H33N3O2S
分子量:487.66
产品类型
结构图
CAS No: 945152-88-5
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产品详情
生物活性:
Antiviral agent 34 is a potent and orally active antiviral agent against influenza A and B subtypes with an EC50 value of 0.8 nM for H1N1 proliferation. Antiviral agent 34 derivatives inhibited influenza virus proliferation by targeting influenza virus RNA-dependent RNA polymerase. Antiviral agent 34 can be used for influenza virus research.
体内研究:
Antiviral agent 34 (Compound 10m) (1 g/kg, 口服给药, 一天三次持续14天) 在致死性流感病毒小鼠模型中显示抗病毒活性。药代动力学分析RouteDose (mg/kg)AUClast (ng?h/mL)AUCINF_obs (ng?h/mL)t1/2 (h)Tmax (h)Cmax (ng/mL)Clobs (L?h/kg)Vss_obs (mL/kg)MRTINF_obs (h)F (%)
i.v.321944219203.690.08419422.29///
p.o.10541653953.264.0d1184///7.38
Animal Model:BALB/c mice
Dosage:1 g/kg/d continues for 14 days
Administration:Oral gavage (p.o.)
Result:Tolerated at a dose of 1 g/kg with low acute toxicity.Provided ~ 50% protection in mice infected with lethal-dose H1N1.
Animal Model:SD rats (Pharmacokinetic assay)
Dosage:3 mg/kg, 10 mg/kg
Administration:intravenous injection (i.v.), oral administration (p.o.)
Result:Had preferable AUC value and low clearance rate and displayed superior oral bioavailability (F = 7.38%).
体外研究:
Antiviral agent 34 (Compound 10m) (0-470 nM, 24 小时) 具有高生物安全性,能抑制 H1N1 病毒增殖。