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ApexBio/MK-0591/10mM (in 1mL DMSO)/A3609

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¥37440.00
货号:A3609
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品牌:ApexBio
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MK-0591FLAP inhibitor,potent and selective

Catalog No.A3609
SizePriceStock
10mM (in 1mL DMSO)
$263.00
Please Inquire
5mg
$203.00
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10mg
$273.00
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50mg
$1,210.00
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100mg
$1,872.00
Please Inquire

Tel: +1-832-696-8203

Email: sales@apexbt.com

Worldwide Distributors

Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Song, Jiao, et al. "Polypharmacology of Small-Molecule Modulators of the 5-Lipoxygenase Activating Protein (FLAP) Observed via a High-throughput Lipidomics Platform." Journal of biomolecular screening (2015): 1087057115607815.PMID:26442913

Quality Control

Quality Control & MSDS

View current batch:
    Purity = 98.00%
  • COA (Certificate Of Analysis)
  • MSDS (Material Safety Data Sheet)
  • Datasheet

Chemical structure

MK-0591

Related Biological Data

MK-0591

Related Biological Data

MK-0591

Biological Activity

DescriptionMK-0591 is a selective and specific inhibitor of 5-Lipoxygenase-activating protein (FLAP).
TargetsFLAP
IC50

MK-0591 Dilution Calculator

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Chemical Properties

Cas No. 136668-42-3SDF Download SDF
Synonyms Quiflapon;MK0591;MK 0591
Chemical Name 3-[3-tert-butylsulfanyl-1-[(4-chlorophenyl)methyl]-5-(quinolin-2-ylmethoxy)indol-2-yl]-2,2-dimethylpropanoic acid
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
Formula C34H35ClN2O3S M.Wt 587.17
Solubility Soluble in DMSO Storage Store at -20°C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

MK-0591, an analog of MK-886 is a potent and orally active leukotriene biosynthesis inhibitor with an IC50 value of 600 ng/ml. MK-0591(250 mg) nearly completely inhibited systemic leukotriene synthesis (>90%) in whole blood or in patients with active disease, and induced LTB4 synthesis in the target tissue of inflammation. [1]MK-0591 plays as a potential agent for the treatment of asthma and inflammatory bowel disease. MK-0591 specific interacted with 5-lipoxygenase, a membrane protein activating protein FLAP, which is essential for LT synthesis in inflammatory cells. [3]MK-0591 inhibited 96% production of LTB4 in whole blood and 91% that from BAL cells. By contrast, MK-0591 had no effect on airway hyper-responsiveness, ozone-induced bronchoconstriction, or influx of neutrophils into BAL. [4]References:1.Hillingsø 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.

ApexBio的3X FLAG Peptide FLAG标签系统利用与目标蛋白质1融合的短而亲水的8个氨基酸的肽段。FLAG肽与抗体M1结合。结合是钙依赖性方式2还是非依赖性3仍存在争议。该系统的缺点是单克隆抗体纯化基质不如其他基质稳定。通常,可以用特异性单克隆抗体检测小标签。为了改善对FLAG标签的检测,已经开发了3x FLAG系统。这种三级FLAG表位是亲水的,长22个氨基酸,可以检测到高达10 fmol的表达融合蛋白。激烈热球菌的带有FLAG标签的麦芽糖糊精结合蛋白已被结晶4,其晶体质量与未标记蛋白的晶体质量非常相似。 最后,可以通过用肠激酶处理去除FLAG标签,肠激酶对肽序列5的5个C末端氨基酸具有特异性。