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Presatovir {[allProObj[0].p_purity_real_show]}

货号:A254733 同义名: GS-5806

Presatovir is a novel inhibitor of respiratory syncytial virus (RSV) fusion F protein with potent antiviral activity against a broad range of strains, working by binding to F protein on the viral surface.

Presatovir 化学结构 CAS号:1353625-73-6
Presatovir 化学结构
CAS号:1353625-73-6
Presatovir 3D分子结构
CAS号:1353625-73-6
Presatovir 化学结构 CAS号:1353625-73-6
Presatovir 3D分子结构 CAS号:1353625-73-6
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Presatovir 纯度/质量文件 产品仅供科研

货号:A254733 标准纯度: {[allProObj[0].p_purity_real_show]}
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Presatovir 生物活性

描述 Presatovir is an antiviral drug which was developed as a treatment for respiratory syncytial virus(RSV). A mean EC50 = 0.43 nM was found toward a panel of 75 RSV A and B clinical isolates and dose-dependent antiviral efficacy in the cotton rat model of RSV infection. Oral bioavailability in preclinical species ranged from 46 to 100%, with evidence of efficient penetration into lung tissue[3]. Presatovir exhibited potent antiviral activity with a mean EC50 value of 0.35 ± 0.14 nM against a broad range of RSV isolates and a low cytotoxicity in vitro. Presatovir exhibited low cytotoxicity in uninfected HEp-2 cells with a CC50 value of 48,900 ± 5,600 nM. Presatovir blocked entry of RSV into host cells, but did not inhibit binding of RSV to the cell surface in temperature shift experiments. Presatovir inhibited RSV replication with an EC50 value of 0.10 ± 0.05 nM [4].

Presatovir 参考文献

[1]Samuel D, Xing W, et al. GS-5806 inhibits pre- to postfusion conformational changes of the respiratory syncytial virus fusion protein. Antimicrob Agents Chemother. 2015 Nov;59(11):7109-12.

[2]Mackman RL, Sangi M, et al. Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study. J Med Chem. 2015 Feb 26;58(4):1630-1643.

[3]Mackman RL, Sangi M, Sperandio D, Parrish JP, Eisenberg E, Perron M, Hui H, Zhang L, Siegel D, Yang H, Saunders O, Boojamra C, Lee G, Samuel D, Babaoglu K, Carey A, Gilbert BE, Piedra PA, Strickley R, Iwata Q, Hayes J, Stray K, Kinkade A, Theodore D, Jordan R, Desai M, Cihlar T. Discovery of an oral respiratory syncytial virus (RSV) fusion inhibitor (GS-5806) and clinical proof of concept in a human RSV challenge study. J Med Chem. 2015 Feb 26;58(4):1630-43. doi: 10.1021/jm5017768. Epub 2015 Jan 27. PMID: 25574686.

[4]Perron M, Stray K, Kinkade A, Theodore D, Lee G, Eisenberg E, Sangi M, Gilbert BE, Jordan R, Piedra PA, Toms GL, Mackman R, Cihlar T. GS-5806 Inhibits a Broad Range of Respiratory Syncytial Virus Clinical Isolates by Blocking the Virus-Cell Fusion Process. Antimicrob Agents Chemother. 2015 Dec 14;60(3):1264-73. doi: 10.1128/AAC.01497-15. PMID: 26666922; PMCID: PMC4776015.

Presatovir 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.88mL

0.38mL

0.19mL

9.40mL

1.88mL

0.94mL

18.79mL

3.76mL

1.88mL

Presatovir 技术信息

CAS号1353625-73-6
分子式C24H30ClN7O3S
分子量 532.058
别名 GS-5806
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Sealed in dry,2-8°C

溶解度

DMSO: 5 mg/mL(9.4 mM),配合低频超声,并水浴加热至45℃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
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