Ziresovir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ziresovir (AK0529; RO-0529) 是一种口服有效的，选择性呼吸道合胞病毒 (RSV) 融合 (F) 蛋白 (RSV F) 抑制剂。 Ziresovir 显示抗 RSV 活性 (EC50=3 nM)， 并具有药代动力学表现。

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.

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.

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.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.

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JAK/STAT Signaling

STAT

RSV

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1422500-60-4

439.53

C22H25N5O3S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (284.39 mM; 超声助溶 )

Cc1ccc2nc(nc(NCC3(N)COC3)c2c1)N1CCS(=O)(=O)c2ccccc2C1

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(-20℃)

With Ice Pack

≥ 2 years