DiFLAPolin 是高活性的双 5-脂氧合酶激活蛋白(FLAP)/可溶性环氧化物水解酶抑制剂,具有显著的抗炎作用和较高的靶向选择性。它抑制分离的 sEH 的活性,IC50为20?nM。它还抑制完整人单核细胞和中性粒细胞中 5-LOX 产物的形成,IC50分别为 30 和 170 nM。
产品描述
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity.
体外活性
Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s?of? 30 and 170?nM, respectively, and suppressed the activity of isolated sEH (IC50=20?nM).
体内活性
Diflapolin (1-10 mg/kg; i.p.; 30?min before zymosan injection) exhibits potent anti-inflammatory properties in in-vivo experiments
Cas No.
724453-98-9
分子式
C22H17Cl2N3O2S
分子量
458.36
储存和溶解度
DMSO:84mg/mL (183.26mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years