| Bioactivity | LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections[1]. |
| Target | IC50: 8.7 μM (LasB) |
| Invitro | LasB-IN-1 (5-10 μM, 10 h) 剂量依赖性地抑制铜绿假单胞菌 PAO1 株中 LasB (IC50 = 8.7 μM) 的表达、弹性酶的生物合成 (IC50 = 7.3 μM) 和生物膜的形成 (IC50 = 7.4 μM) [1]。LasB-IN-1 (1.25-20 μM, 24 h) 对 RAW264.7 细胞和 Vero 细胞无细胞毒作用。LasB-IN-1 (50-100 μM, 24 h) 表现出轻微的细胞毒作用。LasB-IN-1 (0.625-10 μM, 4 h) 对小鼠和人红细胞的溶血作用可忽略不计[1]。LasB-IN-1 (10 μM, 4, 6 h) 能有效抑制斑马鱼幼鱼巨噬细胞向损伤部位的迁移[1]。LasB-IN-1 (0.625-10 μM, 27 h) 抑制 LPS (1 μg/mL, 24 h) 处理的 RAW264.7 细胞 中 IL-1β、TNF-α 和 IL-6 的产生。LasB-IN-1 (1.25-10 μM, 27 h) 也能抑制 COX-2、iNOS、IL-1β、TNF-α 和 IL-6 的 mRNA 表达[1]。LasB-IN-1 (1.25-10 μM, 27 h) 显著抑制 LPS (1 μg/mL, 24 h) 处理的 RAW264.7 细胞内 NF-κB p65、i -κB α、JNK 和 ERK 的磷酸化，且呈浓度依赖性[1]。 0 --> LasB-IN-1 相关抗体: Cell Viability Assay[1] Cell Line: |
| In Vivo | LasB-IN-1 (1, 2 mg/kg, 灌胃, 4 h) 抑制小鼠肺组织内的中性粒细胞浸润[1]。LasB-IN-1 (1, 2 mg/kg, 灌胃, 4 h) 显著下调小鼠 IL-1β、TNF-α 和 IL-6 的表达水平，并降低 COX-2、iNOS、IL-1β、TNF-α 和 IL-6 mRNA 的表达[1]。LasB-IN-1 (2, 4 mg/kg, 灌胃, 每日一次，7 d) 无明显不良反应[1]。 Animal Model: |
| Name | LasB-IN-1 |
| Formula | C20H22F3NO2 |
| Molar Mass | 365.39 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Ping-Hua Sun, et al. Novel ligustilide derivatives target quorum sensing system LasR/LasB and relieve inflammatory response against Pseudomonas aeruginosa infection. European Journal of Medicinal Chemistry. 2023，263，115972. |