Presatovir

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Presatovir (GS-5806) 是一种新型口服生物可利用的 RSV 融合抑制剂（平均 EC50：0.43 nM）。Presatovir 对多种 RSV A 和 B 临床分离株表现出有效的活性（平均 EC50：0.43 nM）。 GS-5806 抑制 RSV F 蛋白前后触发的构象变化，这表明抗病毒活性的可能机制。

Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor (mean EC50: 0.43 nM).Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates (mean EC50: 0.43 nM). GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity.In a cotton rat model of RSV infection, Presatovir demonstrates dose-dependent (0-30 mg/kg) antiviral efficacy. 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 are observed in the high dose group.(In Vitro):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.(In Vivo):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.

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.

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.

GS-5806

Others

Other Targets

RSV

Infection

Respiratory syncytial virus infections

1353625-73-6

532.06

C24H29ClN7O3S

>98% (HPLC)

DMSO:5 mg/mL (9.4 mM; Need ultrasonic and warming);Water:Insoluble

Cc1cn2nc(cc2nc1N1CC[C@H](N)C1)[C@@H]1CCCCN1C(=O)c1cc(Cl)ccc1NS(C)(=O)=O

——

(-20℃)

With Ice Pack

≥ 2 years