MK-0591
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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[1]。
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[3]。
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[4]。
参考文献:
1. Hillings J, Kjeldsen J, Laursen LS et al. Blockade of leukotriene production by a single oral dose of MK-0591 in active ulcerative colitis. Clin Pharmacol Ther. 1995 Mar;57(3):335-41.
2. Prasit P, Belley M, Blouin M et al. A new class of leukotriene biosynthesis inhibitor: the development of MK-0591. J Lipid Mediat. 1993 Mar-Apr;6(1-3):239-44.
3. Stevens WH, Lane CG, Woolley MJ et al. Effect of FLAP antagonist MK-0591 on leukotriene production and ozone-induced airway responses in dogs. J Appl Physiol (1985). 1994 Apr;76(4):1583-8.
Storage | Store at -20°C |
M.Wt | 587.17 |
Cas No. | 136668-42-3 |
Formula | C34H35ClN2O3S |
Synonyms | Quiflapon;MK0591;MK 0591 |
Solubility | Soluble in DMSO |
Chemical Name | 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid |
SDF | Download SDF |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | MK-0591是5-脂氧合酶激活蛋白(FLAP)选择性抑制剂。 | |||||
靶点 | FLAP | |||||
IC50 |