| Description |
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[1].
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| Related Catalog |
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| Target |
IC50: 0.06±0.004 μM (polymerase); EC50: 0.03 μM (influenza A virus)[1]
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| In Vitro |
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[1]。
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| In Vivo |
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[1]。 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[1]。 Animal Model: Balb/C mice[1] 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)[1] 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).
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| References |
[1]. Wang S, et al. Synthesis and structure-activity optimization of 7-azaindoles containing aza-β-amino acids targeting the influenza PB2 subunit. Eur J Med Chem. 2023 Mar 15;250:115185.
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