Pritelivir 是一种病毒解旋酶-引物酶复合物抑制剂,有抗病毒活性。它对 HSV-1 和 HSV-2 具有活性,IC50值为 20 nM。
半岛bd体育手机客户端 描述
Pritelivir (BAY 57-1293) is a potent helicase-primase inhibitor with active against HSV-1 and HSV-2 (IC50: 20 nM).
体外活性
在小鼠和大鼠致死性散播疱疹发病模型、小鼠带状疱疹样皮肤疾病扩散模型中,BAY57-1293(0.5/15 mg/kg,p.o.)均具有较强的抗病毒活性.在小鼠眼疱疹模型中也是如此.
体内活性
BAY57-1293剂量依赖的直接抑制病毒解旋酶-引发酶复合物的ATPase活性。BAY57-1293对耐阿昔洛韦的单纯疱疹病毒突变体也有明显的抗病毒活性。在绿猴肾细胞中,其还可降低1型单纯性疱疹病毒引起的Aβ和P-tau。
激酶实验
In vitro procaspase-3 activation: Procaspase-3 is expressed and purified in Escherichia coli. Various concentrations of PAC-1 are added to 90 μL of a 50 ng/mL of procaspase-3 in caspase assay buffer in a 96-well plate, The plate is incubated for 12 hours at 37 °C. A 10 μL volume of a 2 mM solution of caspase-3 peptidic substrate acetyl Asp-Glu-Val-Asp-p-nitroanilide (Ac-DEVD-pNa) in caspase assay buffer is then added to each well. The plate is read every 2 minutes at 405 nm for 2 hours in a Spectra Max Plus 384 well plate reader. The slope of the linear portion for each well is determined, and the relative increase in activation from untreated control wells is calculated.
Cas No.
348086-71-5
分子式
C18H18N4O3S2
分子量
402.49
别名
BAY 57-1293;AIC316;普瑞利韦
储存和溶解度
DMSO:74 mg/mL (183.9 mM)
H2O:<1 mgml
Ethanol:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years