Leukotriene Receptor Inhibitor

12(S)-HEPE is a monohydroxy fatty acid synthesized from EPA by the action of 12-LO. Unstimulated neutrophils metabolize 12(S)-HEPE to 12(S),20-diHEPE, whereas stimulated neutrophils produce 5(S),12(S)-HEPE via the 5-lipoxygenase pathway. The competitive action of 12(S)-HEPE with arachidonic acid as a substrate for 5-LO in the formation of leukotrienes may provide a basis for the anti-inflammatory potential of ω-3 fatty acids.

JNJ-40929837 is a selective and orally active LTA₄H (leukotriene A₄ hydrolase) inhibitor. JNJ-40929837 effectively inhibits aminopeptidase activity and causes serum accumulation of Pro-Gly-Pro. JNJ-40929837 can be used in asthma research.

(S)-Verapamil-d₇ (hydrochloride) is a deuterium labeled (S)-Verapamil hydrochloride. (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.

Sch 33303 is an orally active antiallergy agent that inhibits the release of the sulfidopeptide leukotrienes. Sch 33303 is promising for research of asthma.

2-ARA-LysoPtdEtn (1-Lyso-2-arachidonoyl-sn-glycero-3-phosphoethanolamine) is an orally active polyunsaturated acyl lysophosphatidylethanolamine. 2-ARA-LysoPtdEtn diminishes formation of LTC₄, LTB₄, and 12-HETE. 2-ARA-LysoPtdEtn lowers levels of IL-1β, IL-6, TNF-α, and NO. 2-ARA-LysoPtdEtn augments IL-10 levels and upgrades formation of 15-HETE and LXA₄. 2-ARA-LysoPtdEtn can be used for the research of peritonitis.

E 6080 is an orally active and selective 5-lipoxygenase (5-LOX) inhibitor with an IC₅₀ of 0.2 μM in rat basophilic leukemia cell. E 6080 shows potent inhibitory effects on the release of leukotrienes. E 6080 inhibits the bronchospasm induced by antigen (ovalbumin) inhalation in sensitized conscious guinea pigs. E 6080 can be used for the study of asthma.

JNJ-40929837 succinate is a selective and orally active LTA₄H (leukotriene A₄ hydrolase) inhibitor. JNJ-40929837 succinate effectively inhibits aminopeptidase activity and causes serum accumulation of Pro-Gly-Pro. JNJ-40929837 succinate can be used in asthma research.

AZD6642 is a 5-lipoxygenase activating protein (FLAP) inhibitor. AZD6642 can effectively inhibit the production of LTB₄. AZD6642 exhibits high oral bioavailability in rats and dogs. AZD6642 can be used in the research of inflammatory diseases.

(R)-Ontazolast ((R)-BIRM-270) is a potent inhibitor of leukotriene biosynthesis, effectively blocking the release of arachidonic acid and demonstrating an impressive IC50 value of 0.001 microM in human polymorphonuclear leukocytes.

Zafirlukast metabolite M1 (compound 15) is an inhibitor of allergic lung diseases such as asthma and can antagonize the activity of leukotrienes.

Chamazulene, a natural compound, is an antioxidant-type inhibitor of leukotriene B4 formation.

ZM 230487 (ICI-230487) is an orally active, selective, non-redox 5-lipoxygenase (5-LO) inhibitor. ZM 230487 potently inhibits antigen-induced LTD₄ release (IC₅₀ ≈ 0.2 µM), but does not affect the release of TXB₂ and histamine. ZM 230487 specifically blocks eosinophil accumulation and partial bronchoconstriction in guinea pig models. ZM 230487 can be used in studies related to allergic inflammation.

LTB4-IN-2 (Comopund 6x) is a Leukotriene B4 (LTB4) inhibitor. LTB4-IN-2 inhibits Leukotriene B4 formation (IC₅₀: 1.15 μM) by selectively targeting 5-Lipoxygenase-activating protein (FLAP). LTB4-IN-2 can be used for anti-inflammatory research.

FK-664 is a leukotriene inhibitor. FK-664 enhances ventricular contractility and shortens the time to peak tension in cardiac cells. FK-664 reduces mean circulating pressure (MCP) in a canine model of heart failure. FK-664 can be used in research on cardiovascular diseases such as heart failure.

L-691678 can bind to FLAP by recognizing the amino acid residues of 5-lipoxygenase-activating protein (FLAP), thereby inhibiting leukotriene biosynthesis. L-691678 can be used in the study of leukotriene-related diseases such as allergies, asthma, and inflammation.

Nedocromil (Standard) is the analytical standard of Nedocromil. This product is intended for research and analytical applications. Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C₄ (LTC₄), and prostaglandin D₂ (PGD₂).

Darbufelone (mesylate) (Standard) is the analytical standard of Darbufelone (mesylate) (HY-101438A). This product is intended for research and analytical applications. Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).

NPC-18915 free base is a neutrophil activation inhibitor. NPC-18915 free base inhibits CD11b/CD18-mediated neutrophil adhesion. NPC-18915 free base induces shedding of L-selectin on the neutrophil surface, thereby reducing endothelial cell adhesion. NPC-18915 free base inhibits calcium ionophore-induced LTB₄ synthesis in neutrophils. NPC-18915 free base reduces the severity of TNBS-induced acute and recurrent colitis in rat experiments. NPC-18915 free base can be used in studies related to colitis.

11-Keto-beta-boswellic acid (Standard) is the analytical standard of 11-?Keto-?beta-?boswellic acid. This product is intended for research and analytical applications. 11-Keto-beta-boswellic acid (11-Keto-β-boswellic acid) is a pentacyclic triterpenic acid of the oleogum resin from the bark of the Boswellia serrate tree, popularly known as Indian Frankincense. 11-Keto-beta-boswellic acid has the anti-inflammatory activity is primarily due to inhibit 5-lipoxygenase (5-LOX) and subsequent leukotriene and nuclear factor-kappa B (NF-κB) activation and tumor necrosis factor alpha generation production.

MK-886 (Standard) is the analytical standard of MK-886. This product is intended for research and analytical applications. MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis.