产品说明书

Presatovir

Print
Chemical Structure| 1353625-73-6 同义名 : GS-5806
CAS号 : 1353625-73-6
货号 : A254733
分子式 : C24H30ClN7O3S
纯度 : 99%+
分子量 : 532.058
MDL号 : MFCD28963961
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.