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抑制剂描述:

产品名称:Presatovir

产品别名:见爱必信

英文别名:Presatovir

靶点:HSV

CAS:1353625-73-6

纯度:>98%

外观:见爱必信

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Presatovir is a novel, orally bioavailable RSV fusion inhibitor, against a wide range of RSV A and B clinical isolates (mean EC50 = 0.43 nM).

溶解性:DMSO : 6 mg/mL (11.28 mM; Need ultrasonic and warming)

体外研究:

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. GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity.

体内研究: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 , with penetration of the compound into the lung tissue demonstrated in Sprague-Dawley rats. Multidose oral treatment of Presatovir appears safe , 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.

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