产品名称

英文名称：MK-0591

同义词

Quiflapon、136668-42-3、MK-0591、Quiflapon [INN]、Quiflapon free acid、MK 0591、3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid、MK 591、3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-y

产品性质

CAS编号：136668-42-3

分子式：C34H35ClN2O3S

分子量：587.17

PubChem编号：60923

英文别名：Quiflapon|136668-42-3|MK-0591|Quiflapon [INN]|Quiflapon free acid|MK 0591|3-(3-(tert-butylthio)-1-(4-chlorobenzyl)-5-(quinolin-2-ylmethoxy)-1H-indol-2-yl)-2,2-dimethylpropanoic acid|MK 591|3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-y

规格或纯度：98%

英文名称：MK-0591

生化机理：MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. MK-0591 is a synthetic compound which specifically inhibits the activity of 5-Lox and is currently under development for the treatment of asthma. Research of involvement of 5-lipoxygenase activating protein in the amyloidotic phenotype of an Alzheimer's disease mouse model showed that a novel functional role for 5-lipoxygenase activating protein in the pathogenesis of Alzheimer's disease-like amyloidosis, and sμggest that its pharmacological inhibition could provide a novel therapeutic opportunity for Alzheimer's disease. Another research showed 5-Lipoxygenase-activating protein (FLAP) inhibitor MK-0591 prevents aberrant alveolarization in newborn mice exposed to 85% oxygen in a dose- and time-dependent manner.

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：产品介绍Quiflapon (MK-591)是一种选择性和特异性的 FLAP 抑制剂，IC50 为 1.6 nM。Quiflapon 也是一种有效的白三烯生物合成 (leukotriene biosynthesis) 抑制剂，在完整的人和诱导的大鼠多形核白细胞 PMNLs 中，其 IC50 值分别为 3.1 nM 和 6.1 nM。Quiflapon 可以诱导细胞凋亡 (apoptosis)。MK-0591，一种MK-886类似物，是有效的和可口服的白三烯生物合成抑制剂，其IC50值为600 ng/ml。MK-0591（250 mg）几乎完全抑制全血或活动性疾病患者中全身性白三烯合成（>90％），并诱导炎症靶组织合成LTB4。MK-0591是一种治疗哮喘和炎症性肠病的潜在药物。MK-0591特异性地结合5-脂氧合酶（一种膜蛋白激活蛋白FLAP），两者的相互作用是炎性细胞合成LT的必要条件。在全血以及BAL细胞中，MK-0591分别抑制了96%和91%的LTB4合成。与此相反，MK-0591不影响气道高反应性、臭氧引起的支气管收缩或嗜中性粒细胞向BAL细胞的流入。

IUPAC Name：3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid

INCHI：InChI=1S/C34H35ClN2O3S/c1-33(2,3)41-31-27-18-26(40-21-25-15-12-23-8-6-7-9-28(23)36-25)16-17-29(27)37(20-22-10-13-24(35)14-11-22)30(31)19-34(4,5)32(38)39/h6-18H,19-21H2,1-5H3,(H,38,39)

InChi Key：NZOONKHCNQFYCI-UHFFFAOYSA-N

Canonical SMILES：CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)CC5=CC=C(C=C5)Cl)CC(C)(C)C(=O)O

Isomeric SMILES：CC(C)(C)SC1=C(N(C2=C1C=C(C=C2)OCC3=NC4=CC=CC=C4C=C3)CC5=CC=C(C=C5)Cl)CC(C)(C)C(=O)O

PubChem CID：60923

溶解性：DMSO

产品包装