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Presatovir(GS-5806)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Presatovir(GS-5806)图片
CAS NO:1353625-73-6
规格:98%
分子量:532.06
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
Presatovir(GS-5806)是新颖且有口服活性的RSV融合抑制剂,平均EC50值为0.43nM.
CAS:1353625-73-6
分子式:C24H30ClN7O3S
分子量:532.06
纯度:98%
存储:Store at -20°C

Background:

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM.


Presatovir is a novel, orally bioavailable RSV fusion inhibitor discovered following a lead optimization campaign on a hit originated from a phenotypic RSV antiviral high-throughput screen. Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates with a mean EC50 value of 0.43 nM[1]. GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity[2].


Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy in a cotton rat model of RSV infection. Oral bioavailability in preclinical species ranges from 46 to 100%, with penetration of the compound into the lung tissue demonstrated in Sprague-Dawley rats. Multidose oral treatment of Presatovir appears safe in adults, and in healthy human volunteers experimentally infected with RSV, a potent antiviral effect and reduction in disease severity is observed in the high dose group. A group treated with a lower dose of Presatovir allows for a PK-PD relationship to be established to help guide future dose selections[1].


[1]. Mackman RL, 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. [2]. Samuel D, 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.