普沙托韦 TQ0085

Product Introduction
Bioactivity


英文名: Presatovir

描述: Presatovir (GS-5806) 是一种新型的口服生物可利用的 RSV 融合抑制剂，平均 EC50值为 0.43 nM。

细胞实验: GS-5806 is diluted in 100% DMSO. To conduct the cytopathic antiviral assay, 0.4 μL of 100×concentrated 3-fold serially diluted drug is added to 20 μL of cell culture medium in a 384-well plate. HEp-2 cells are then suspended in MEM plus 10% FBS at a density of 1×10^5 cells/mL, are infected in bulk with RSV A2 at a titer of approximately 1×10^4.5 tissue culture infectious doses/mL. Immediately following infection, 20 μL of RSV-infected cells are added to each well. The cells are then cultured for 4 days at 37 °C. Following this incubation, the cells are allowed to equilibrate to 25°C. The RSV-induced cytopathic effect is determined by adding 40 μL of Cell-Titer Glo viability reagent. Following a 10 min incubation at 25 °C, cell viability is determined [1].

体外活性: Presatovir exhibits potent activity against a wide range of RSV A and B clinical isolates (mean EC50: 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].

体内活性: 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 [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 5 mg/mL (9.4 mM)
H2O : Insoluble


关键字: inhibit | Inhibitor | Respiratory syncytial virus | GS 5806 | GS5806 | Presatovir | RSV

相关产品: Palivizumab | VV116 | GS-443902 | RSV604 | Suptavumab | RSV L-protein-IN-4 | Rilematovir | 4-Methoxycinnamaldehyde | JNJ-8003 | Roflumilast

相关库: Drug Repurposing Compound Library | ReFRAME Related Library | Clinical Compound Library | Inhibitor Library | Pediatric Drug Library | Orally Active Compound Library | Anti-Viral Compound Library | NO PAINS Compound Library | Bioactive Compound Library | Anti-Infection Compound Library

普沙托韦 TQ0085信息由TargetMol中国为您提供，如您想了解更多关于普沙托韦 TQ0085报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途