Docebenone(AA861)是一种有效的、选择性的和有口服活性的5-脂氧合酶(5-LO)抑制剂。
货号:ajcx12708
CAS:80809-81-0
分子式:C21H26O3
分子量：326.43
溶解度:DMSO: 250 mg/mL (765.86 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.

Treatment of trichomonads with the 5-LO inhibitor Docebenone, significantly inhibits the ability of trichomonads to secrete LTB4 compared to results for trichomonads treated with medium. Docebenone strongly abolishes the stimulatory effect of TvSP on IL-8 production[1]. Docebenone at 10-200 μM increases [Ca2+]i concentration dependently[2].

Docebenone might protect experimental acute necrotizing pancreatitis in rats[3]. Docebenone suppresses the release of SRS-A by 55-97%, dose-dependently in doses of 10-8-10-5 M in monkeys. The antigen-induced SRS-A release from these fragments is dose dependently inhibited by 25-93% of Docebenone, with doses of 10-8-10-5 M[4].

[1]. Nam YH, et al. Leukotriene B(4) receptors BLT1 and BLT2 are involved in interleukin-8 production in human neutrophils induced by Trichomonas vaginalis-derived secretory products. Inflamm Res. 2012 Feb;61(2):97-102. [2]. Huang JK, et al. AA-861-induced Ca(2+) mobilization in Madin Darby canine kidney cells. Toxicol Appl Pharmacol. 1999 Dec 1;161(2):202-8. [3]. Kiriyama M, et al. Protective effect of AA-861 (5-lipoxygenase inhibitor) on experimental acute necrotizing pancreatitis in rats. Int J Pancreatol. 1993 Jun;13(3):201-8. [4]. Yamamura H, et al. Effect of AA-861, a selective 5-lipoxygenase inhibitor, on models of allergy in several species. Jpn J Pharmacol. 1988 Jul;47(3):261-71.

Protocol:

Animal experiment:

Rats[3]Pancreatitis is induced in rats by retrograde injection of 0.4 mL/kg body wt of 6% taurocholic acid into the pancreatic duct. The animals are divided into three groups: control group; administered Docebenone in a single dose of 30 mg/kg; and administered Docebenone in a single dose of 60 mg/kg. The following parameters are examined: serum amylase, lipase, trypsin, blood sugar, and survival rate[3].

参考文献: [1]. Nam YH, et al. Leukotriene B(4) receptors BLT1 and BLT2 are involved in interleukin-8 production in human neutrophils induced by Trichomonas vaginalis-derived secretory products. Inflamm Res. 2012 Feb;61(2):97-102. [2]. Huang JK, et al. AA-861-induced Ca(2+) mobilization in Madin Darby canine kidney cells. Toxicol Appl Pharmacol. 1999 Dec 1;161(2):202-8. [3]. Kiriyama M, et al. Protective effect of AA-861 (5-lipoxygenase inhibitor) on experimental acute necrotizing pancreatitis in rats. Int J Pancreatol. 1993 Jun;13(3):201-8. [4]. Yamamura H, et al. Effect of AA-861, a selective 5-lipoxygenase inhibitor, on models of allergy in several species. Jpn J Pharmacol. 1988 Jul;47(3):261-71.