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编 号:F157505
分子式:C22H25N5O3S
分子量:439.53
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
Ziresovir (AK0529;RO-0529) is a potent, selective, and orally bioavailable respiratory syncytial virus (RSV) fusion (F) protein (RSV F) protein inhibitor. Ziresovir shows anti-RSV activity (EC50=3 nM) and highlights pharmacokinetics in animal species.

体内研究:
Ziresovir (12.5 mg/kg, 50 mg/kg; p.o.; twice daily; 4 d) results reduction of RSV titer in mouse lung. Ziresovir (10 mg/kg; p.o.; single dose) exhibits good oral exposure and bioavailability?with F(%) of 32% in male Wistar-Han rats. Ziresovir (150 mg/kg; p.o.; single dose) demonstrates a high tissue distribution to lung than plasma in CD-1 Mice.Pharmacokinetics of Ziresovir in male Wistar-Han ratsDose (mg/kg)AUC0-24h(p.o.) (ng·h/mL)CL (mL/min/kg)T1/2(i.v.) (h)Vss (L/kg)F (%)
2 mg/kg (iv) or 10 mg/kg (po)906581.23.932
Pharmacokinetics of Ziresovir in CD-1 MiceDose (mg/kg)AUC0-24h(p.o.) (μg·h/L)tissue/lasma AUC0-24h ratio (μg·h/L)T1/2 (h)Tmax (h)Cmax (μg/L)
plasma8,38011.020.255090
lung72,4008.63.31122700
Animal Model:Female BALB/c mice infected by RSV
Dosage:12.5 mg/kg, 50 mg/kg
Administration:Oral gavage; twice daily; 4 days
Result:Resulted >1 log unit of viral titer reduction in the lung of infected mice at the dose level as low as 12.5 mg/kg.?Reduced viral titer to 1.9 log units compared to vehicle at 50 mg/kg dose.

体外研究:
Ziresovir shows different efficacy in Wild Type (WT) and Mutant Strains RSV with EC50/EC90 values (μM) of 0.003/0.005 (WT), 2.1/10.0 (D486N), and >10/>10 (D489A), respectively.RO-0529 (100 nM; 4 d) inhibits RSV F protein-induced cell–cell fusion process, and suppresses the syncytia formation induced by the RSV F protein.
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