Pritelivir (BAY 57-1293) (BAY 57-1293) is a potent helicase-primase inhibitor with active against HSV-1 and HSV-2 (IC50: 20 nM).

HSV1/HSV2:20 nM, HSV2:20 nM

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.

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。

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.