Ziresovir|1422500-60-4|(AK0529; RO-0529)-陌孚医药/Medlife

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Ziresovir (Synonyms: AK0529; RO-0529)

目录号: PL11098 纯度: ≥98.0%

CAS No. :1422500-60-4

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中文名称	Ziresovir
中文别名	N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine
英文名称	Ziresovir
英文别名	N-[(3-aminooxetan-3-yl)methyl]-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine;Ziresovir;XCF42D7AG4;Ziresovir [INN];N-((3-Aminooxetan-3-yl)methyl)-2-(1,1-dioxido-2,3-dihydro-1,4-benzothiazepin-4(5H)-yl)-6-methylquinazolin-4-amine;GAAICKUTDBZCMT-UHFFFAOYSA-N;DB15145;N-((3-Amino-3-oxetanyl)methyl)-2-(2,3-dihydro-1,1-dioxido-1,4-benzothiazepin-4(5H)-yl)-6-methyl-4-quinazolinamine;4-(4-(((3-Aminooxet;AK0529;RO-0529;BDBM50516304;4-(4-(((3-Aminooxetan-3-yl)methyl)amino)-6-methylquinazolin-2-yl)-2,3,4,5-tetrahydro-1H-1lambd
Cas No.	1422500-60-4
分子式	C₂₂H₂₅N₅O₃S
分子量	439.53
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

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。

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 (EC 50 =3 nM) and highlights pharmacokinetics in animal species.

性状

Solid

IC50 & Target[1][2]

RSV F protein (respiratory syncytial virus fusion protein) EC50: 3 nM (RSV F)

体外研究(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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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) AUC 0-24h (p.o.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Zheng X, et al. Discovery of Ziresovir as a Potent, Selective, and Orally Bioavailable Respiratory Syncytial Virus Fusion Protein Inhibitor. J Med Chem. 2019 Jul 11;62(13):6003-6014.

溶解度数据	In Vitro: DMSO : 125 mg/mL (284.39 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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