Diflapolin, 环氧化物水解酶 2 抑制剂

小分子

迪弗林

Diflapolin

D656372-1ml

1ml

Moligand™

10mM in DMSO

-80℃储存

超低温冰袋运输

Diflapolin 是一种高活性的双 5-脂氧合酶激活蛋白 (FLAP)/可溶性环氧化物水解酶 (sEH) 抑制剂，具有显著的抗炎作用和较高的靶向选择性。Diflapolin 抑制 IC50 分别为 30 和 170 nM 的完整人单核细胞和中性粒细胞中 5-LOX 产物的形成，并抑制分离的 sEH 的活性(IC50=20 nM)。 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. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC 50 s of 30 and 170 nM, respectively, and suppressed the activity of isolated sEH ( IC 50 =20 nM). In Vivo Diflapolin (1-10 mg/kg; i.p.; 30 min before zymosan injection) exhibits potent anti-inflammatory properties in in-vivo experiments . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD-1 mice (zymosan-induced peritonitis mouse model) Dosage: 1, 3 and 10 mg/kg Administration: I.p.; 30 min before zymosan injection Result: Induced a significant reduction of LTC4 and LTB4 peritoneal levels, starting from the dose of 1 mg/kg and comparable to the effect of MK886.

Diflapolin 是一种高活性的 5-Lipoxygenase-activating protein（FLAP）/soluble epoxide hydrolase（sEH）双重抑制剂，具有显著的抗炎功效和高度的靶标选择性。Diflapolin 可抑制完整人单核细胞中 5-LOX 产物的形成

724453-98-9(DMSO)

C22H17Cl2N3O2S

458.4 g/mol

CC1=C(C=CC(=C1)OCC2=NC3=CC=CC=C3S2)NC(=O)NC4=CC(=C(C=C4)Cl)Cl

抑制剂

环氧化物水解酶 2 抑制剂