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- 详细信息
- 技术资料
- 保存条件:
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 英文名:
AK0529; RO-0529
- 库存:
货期:1-2天
- 供应商:
MedChemExpress LLC
- CAS号:
1422500-60-4
- 规格:
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格: | 10 mM * 1 mL | 产品价格: | ¥3384.0 |
|---|---|---|---|
| 规格: | 1 mg | 产品价格: | ¥1591.0 |
| 规格: | 5 mg | 产品价格: | ¥3500.0 |
| 规格: | 10 mg | 产品价格: | ¥5100.0 |
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Ziresovir
CAS No. : 1422500-60-4
MCE 国际站:Ziresovir
产品活性: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。
研究领域:Anti-infection
作用靶点:RSV
In Vitro: 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.
In Vivo: 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 rats
| Dose (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) | 906 | 58 | 1.2 | 3.9 | 32 |
| Dose (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) |
| plasma | 8,380 | 1 | 1.02 | 0.25 | 5090 |
| lung | 72,400 | 8.6 | 3.31 | 1 | 22700 |
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