Presatovir (GS-5806) 是新颖且有口服活性的 RSV 融合抑制剂,平均EC50 值为0.43 nM.
Description | Presatovir (GS-5806) is a novel, orally bioavailable RSV fusion inhibitor with a mean EC50 value of 0.43 nM. | ||||||||||||||||
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IC50 & Target | EC50: 0.43 nM (RSV)[1] | ||||||||||||||||
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[1]. GS-5806 inhibits pre to post triggered conformational changes of RSV F protein, suggesting a possible mechanism for antiviral activity[2]. | ||||||||||||||||
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[1]. | ||||||||||||||||
Solvent & Solubility | In Vitro: DMSO : 6 mg/mL (11.28 mM; Need ultrasonic and warming) H2O : < 0.1 mg/mL (insoluble) Preparing Stock Solutions
* Please refer to the solubility information to select the appropriate solvent. In Vivo:
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