118414-82-7 | MK-886

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$12.00	$9.00
5mg	98%	in stock	$26.00	$18.00
10mg	98%	in stock	$37.00	$26.00
25mg	98%	in stock	$62.00	$44.00

Description

• Catalog Number: AE08874
• Chemical Name: MK-886
• CAS Number: 118414-82-7
• Molecular Formula: C27H34ClNO2S
• Molecular Weight: 472.0824
• MDL Number: MFCD00876710
• SMILES: Clc1ccc(cc1)Cn1c2ccc(cc2c(c1CC(C(=O)O)(C)C)SC(C)(C)C)C(C)C
• NSC Number: 736463

Computed Properties

• Complexity: 638
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 32
• Hydrogen Bond Acceptor Count: 3
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 8
• XLogP3: 7.6

Upstream Synthesis Route

MK-886 is a potent and selective inhibitor of the enzyme 5-lipoxygenase-activating protein (FLAP), which plays a crucial role in the biosynthesis of leukotrienes. Leukotrienes are inflammatory mediators derived from arachidonic acid and are involved in various physiological and pathological processes. In the field of chemical synthesis, MK-886 is utilized as a valuable tool in the study of leukotriene biosynthesis and related pathways. By inhibiting FLAP, MK-886 helps researchers investigate the specific roles of leukotrienes in inflammation, immune responses, and respiratory diseases. Additionally, MK-886 can be used to explore potential therapeutic interventions targeting the leukotriene pathway. Its efficacy and selectivity make MK-886 a valuable asset in unraveling the complexities of leukotriene biology and in developing targeted drug therapies for conditions influenced by leukotriene activity.

Literature

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  The Journal of pharmacology and experimental therapeutics 20051101

• Mast cell mediators in citric acid-induced airway constriction of guinea pigs.

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  Cancer research 20050515

• Induced microsomal PGE synthase-1 is involved in cyclooxygenase-2-dependent PGE2 production in gastric fibroblasts.

  American journal of physiology. Gastrointestinal and liver physiology 20050201

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  In vivo (Athens, Greece) 20050101

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• Non-prostaglandin eicosanoids in fever and anapyrexia.

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  European journal of pharmacology 20040816

• Interleukin-18 induces mechanical hypernociception in rats via endothelin acting on ETB receptors in a morphine-sensitive manner.

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  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20040501

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• Inflammatory response of human tendon fibroblasts to cyclic mechanical stretching.

  The American journal of sports medicine 20040301

• Molecular mechanism of nucleotide-induced primary granule release in human neutrophils: role for the P2Y2 receptor.

  American journal of physiology. Cell physiology 20040201

• Leukotrienes-mediated effects of water extracts from Sargassum horneri, a marine brown alga, on Cl- absorption in isolated rat colon.

  The Japanese journal of physiology 20040201

• Nicotine promoted colon cancer growth via epidermal growth factor receptor, c-Src, and 5-lipoxygenase-mediated signal pathway.

  The Journal of pharmacology and experimental therapeutics 20040101

• Five-lipoxygenase-activating protein inhibitor MK-886 induces apoptosis in gastric cancer through upregulation of p27kip1 and bax.

  Journal of gastroenterology and hepatology 20040101

• Membrane-associated prostaglandin E synthase-1 is upregulated by proinflammatory cytokines in chondrocytes from patients with osteoarthritis.

  Arthritis research & therapy 20040101

• Acute changes in U937 nuclear Ca2+ preceding type 1 'apoptotic' programmed cell death due to MK 886.

  Anticancer research 20040101

• Molecular and catalytic properties of three rat leukotriene C(4) synthase homologs.

  Biochemical and biophysical research communications 20031212

• Expression of lipoxygenase in human bladder carcinoma and growth inhibition by its inhibitors.

  The Journal of urology 20031101

• NFkappaB regulates plasma apolipoprotein A-I and high density lipoprotein cholesterol through inhibition of peroxisome proliferator-activated receptor alpha.

  The Journal of biological chemistry 20031003

• Inhibition of leukotriene synthesis with MK-886 prevents a rise in blood pressure and reduces noradrenaline-evoked contraction in L-NAME-treated rats.

  British journal of pharmacology 20030901

• Caspase-dependent and -independent panc-1 cell death due to actinomycin D and MK 886 are additive but increase clonogenic survival.

  Experimental biology and medicine (Maywood, N.J.) 20030901

• 5-Lipoxygenase is involved in the angiotensin II-induced NAD(P)H-oxidase activation.

  Biochemical and biophysical research communications 20030829

• Potentiation of tumor necrosis factor alpha-induced secreted phospholipase A2 (sPLA2)-IIA expression in mesangial cells by an autocrine loop involving sPLA2 and peroxisome proliferator-activated receptor alpha activation.

  The Journal of biological chemistry 20030808

• Roles of 5-lipoxygenase activating protein in cell proliferation and apoptosis.

  Cell biology and toxicology 20030601

• Increased expression of the lipocalin 24p3 as an apoptotic mechanism for MK886.

  The Biochemical journal 20030515

• Microsomal prostaglandin E synthase-1 is a major terminal synthase that is selectively up-regulated during cyclooxygenase-2-dependent prostaglandin E2 production in the rat adjuvant-induced arthritis model.

  Journal of immunology (Baltimore, Md. : 1950) 20030501

• Arachidonic acid in astrocytes blocks Ca(2+) oscillations by inhibiting store-operated Ca(2+) entry, and causes delayed Ca(2+) influx.

  Cell calcium 20030401

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  Cytokine 20030307

• Fatty acid release and oxidation are factors in lipoxygenase inhibitor-induced apoptosis.

  Toxicology letters 20030303

• Leukotriene-mediated coronary vasoconstriction and loss of myocardial contractility evoked by low doses of Escherichia coli hemolysin in perfused rat hearts.

  Critical care medicine 20030301

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  Journal of leukocyte biology 20030301

• Role of downstream metabolic processing of proinflammatory fatty acids by 5-lipoxygenase in HL-60 cell apoptosis.

  The Journal of trauma 20030101

• An interaction between type 1 and type 2 programmed cell death and clonogenic survival.

  Medical hypotheses 20030101

• Spermadhesin PSP-I/PSP-II heterodimer and its isolated subunits induced neutrophil migration into the peritoneal cavity of rats.

  Biology of reproduction 20021201

• 5(S)-Hydroxy-6,8,11,14-E,Z,Z,Z-eicosatetraenoate stimulates PC3 cell signaling and growth by a receptor-dependent mechanism.

  Cancer research 20021201

• The cyclooxygenase inhibitor ibuprofen and the FLAP inhibitor MK886 inhibit pancreatic carcinogenesis induced in hamsters by transplacental exposure to ethanol and the tobacco carcinogen NNK.

  Journal of cancer research and clinical oncology 20021001

• Distinct pathways of lipopolysaccharide priming of human neutrophil respiratory burst: role of lipid mediator synthesis and sensitivity to interleukin-10.

  Critical care medicine 20021001

• Mitochondria are direct targets of the lipoxygenase inhibitor MK886. A strategy for cell killing by combined treatment with MK886 and cyclooxygenase inhibitors.

  The Journal of biological chemistry 20020830

• Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice.

  Cancer research 20020801

• Early vascular permeability in murine experimental peritonitis is co-mediated by resident peritoneal macrophages and mast cells: crucial involvement of macrophage-derived cysteinyl-leukotrienes.

  Inflammation 20020401

• Increased cytosol Ca(2+) and type 1 programmed cell death in Bcl-2-positive U937 but not in Bcl-2-negative PC-3 and Panc-1 cells induced by the 5-lipoxygenase inhibitor MK 886.

  Prostaglandins, leukotrienes, and essential fatty acids 20020401

• Formation of murine macrophage-derived 5-oxo-7-glutathionyl-8,11,14-eicosatrienoic acid (FOG7) is catalyzed by leukotriene C4 synthase.

  The Journal of biological chemistry 20020301

• Potentiation of TNF-alpha-stimulated group IIA phospholipase A(2) expression by peroxisome proliferator-activated receptor alpha activators in rat mesangial cells.

  Journal of the American Society of Nephrology : JASN 20020301

• Leukotriene B4 production in human mononuclear phagocytes is modulated by interleukin-4-induced 15-lipoxygenase.

  The Journal of pharmacology and experimental therapeutics 20020301

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  American journal of physiology. Heart and circulatory physiology 20020201

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• A useful method for differential evaluation of anti-inflammatory effects due to cyclooxygenase and 5-lipoxygenase inhibitions in mice.

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• The 5-lipoxygenase inhibitors ZD2138 and ZM230487 are potent and selective inhibitors of several antigen-induced guinea-pig pulmonary responses.

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• Assessment of the in vivo biochemical efficacy of orally active leukotriene biosynthesis inhibitors.

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• Anti-leukotriene effects of WY-50,295 tromethamine in isolated guinea pig pulmonary tissues.

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• Mode of action of the new selective leukotriene synthesis inhibitor BAY X 1005 ((R)-2-[4-(quinolin-2-yl-methoxy)phenyl]-2-cyclopentyl acetic acid) and structurally related compounds.

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• Requirement of a 5-lipoxygenase-activating protein for leukotriene synthesis.

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