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编 号:F744970
分子式:C17H18F2N6O2
分子量:376.36
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生物活性:
HAA-09 is an orally active and potent anti-influenza agent, targeting the influenza PB2_cap binding domain. HAA-09 displays potent anti-influenza A virus activity, with an EC50 of 0.03 μM. HAA-09 shows polymerase inhibition, with an IC50 of 0.06±0.004 μM. HAA-09 blocks virus replication without causing obvious cytotoxicity.

体内研究:
HAA-09 具有较高的血浆稳定性(t1/2≥12 h),且无明显的 hERG 抑制作用。HAA-09 (0-25 mg/kg; 口服; 每天两次) 在小鼠体内具有抗流感病毒作用。Animal Model:Balb/C mice
Dosage:40 mg/kg
Administration:Orally, QD (once daily) for consecutive 3 days
Result:Demonstrated a favorable safety profile when orally administrated in healthy mice.
Animal Model:Female BALB/c mice (6–8 weeks)
Dosage:12.5, 25 mg/kg
Administration:Orally, BID (twice daily) starting 48 h post infection for 9 days
Result:Demonstrated in vivo therapeutic efficacy (85.7% survival observed at the day 15 post infection).

体外研究:
HAA-09 对奥司他韦 (oseltamivir) 敏感的 A/WSN/33 和奥司他韦耐药的 H275Y 变体表现出更强的抗病毒活性,优于奥司他韦。
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