Baloxavir marboxil

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Chemical Structure| 1985606-14-1 同义名 : -
CAS号 : 1985606-14-1
货号 : A267027
分子式 : C27H23F2N3O7S
纯度 : 97%
分子量 : 571.549
MDL号 : MFCD31619272
存储条件:

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 35 mg/mL(61.24 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Seasonal and pandemic influenza are the two faces of respiratory infections caused by influenza viruses in humans. Influenza virus infection may result in pneumonia and acute respiratory failure, frequently complicated by bacterial coinfection[1]. Baloxavir marboxil is a small molecule inhibitor of the cap-dependent endonuclease of influenza A and B viruses. Baloxavir marboxil is a prodrug that is metabolised to an active form (known as S‐033447) which is highly effective at inhibiting a number of different influenza A and B viruses in vitro[2]. In a mouse model of infection, a single dose of Baloxavir marboxil was found to reduce viral load by 2 logs and reduced mortality compared to mice being treated with oseltamivir. In a phase II study of S‐033188, patients with uncomplicated influenza were randomised to three different doses (10 mg, 20 mg and 40 mg) and compared to placebo. All three doses resulted in significant reductions in time to alleviation of symptoms and reduced virus titres at 24 and 48 hours post‐treatment compared to placebo[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.75mL

0.35mL

0.17mL

8.75mL

1.75mL

0.87mL

17.50mL

3.50mL

1.75mL

参考文献

[1]Peteranderl C, Herold S, Schmoldt C. Human Influenza Virus Infections. Semin Respir Crit Care Med. 2016 Aug;37(4):487-500. doi: 10.1055/s-0036-1584801. Epub 2016 Aug 3. PMID: 27486731; PMCID: PMC7174870.

[2]Koszalka P, Tilmanis D, Hurt AC. Influenza antivirals currently in late-phase clinical trial. Influenza Other Respir Viruses. 2017 May;11(3):240-246. doi: 10.1111/irv.12446. Epub 2017 Feb 28. PMID: 28146320; PMCID: PMC5410715.