Leukotriene Receptor Inhibitor

Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF_2α and LTB₄ production. Darbufelone potently inhibits PGHS-2 (IC₅₀ = 0.19 μM) but is much less potent with PGHS-1 (IC₅₀= 20 μM).

Tryptanthrin (Standard) is the analytical standard of Tryptanthrin. This product is intended for research and analytical applications. Tryptanthrin is an indole quinazoline that could be an alkaloid from indigo-bearing plants. Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin has anticancer activity. Tryptanthrin suppresses the expression levels of NOS1, COX-2, and NF-κB and regulates the expression levels of IL-2, IL-10, and TNF-α.

L-674573 is a quinoline leukotriene synthesis inhibitor, inhibiting Calcimycin (HY-N6687)- and N-Formyl-Met-Leu-Phe (HY-P0224)-induced leukotriene production with IC₅₀s of 100 nM and 50 nM, respectively. L-674573 selectively inhibits Calcimycin- and N-Formyl-Met-Leu-Phe-induced 5-lipoxygenase translocation.

MK-886 (L 663536) sodium salt 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 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis.

BLT1-IN-1 is an orally active and selective BLT1 inhibitor with an IC₅₀ of 8.7 nM and a K_d of 121 nM. BLT1-IN-1 exerts protective effects against acute lung injury and sepsis in in vivo models. BLT1-IN-1 can be used in research related to acute lung injury and sepsis.

Enofelast (BI-L-239), a 5-lipoxygenase (5-LO) inhibitor, exhibits an IC₅₀ of 2.48 μM for inhibition of calcium ionophore-induced LTB₄ generation.

Nyasol ((-)-Nyasol) is an active compound that has antifungal, antibacterial, antileishmanial, hyaluronidase inhibition activities. Nyasol inhibits LTB4 binding to human neutrophils. Nyasol suppresses neuroinflammatory response through the inhibition of I-κB degradation in LPS (HY-D1056)-stimulated BV-2 microglial cells.

Pirodomast (Sch 37224) is a leukotriene formation inhibitor. Pirodomast inhibits LTD4 andthromboxane B2 release by anaphylactic guinea pig lung with the IC₅₀ values of 3.9 and 1.9 μM, respectively. Pirodomast can be used for study of asthma.

ZPL-5212372 (PF 5212372) is a cPLA2α inhibitor (IC₅₀ = 7 nM). ZPL-5212372 inhibits the release of prostaglandin D2 (PGD2), cysteyl leukotrienes, leukotriene B4, thromboxane A2, and PGD2 from human lung cells. ZPL-5212372 inhibits delayed bronchoconstriction and airway hyperresponsiveness in a sheep allergic inflammation model. ZPL-5212372 may be used in asthma research.

PL265 is an orally active dual enkephalinase inhibitor. PL265 is a prodrug of PL254, which can simultaneously and efficiently inhibit neutral endopeptidase (Neprilysin) and Aminopeptidase N. PL265 can effectively protect and significantly increase the local concentration of enkephalins (such as Met-Enkephalin and Leu-Enkephalin) released by cells at the pain or inflammation sites, thereby activating μ and δ opioid receptors to produce a potent analgesic effect. PL254 can also inhibit leukotriene A4 hydrolase (LTA4H), which may contribute to its additional anti-inflammatory effect by reducing the production of pro-inflammatory mediator leukotriene B4 (LTB4). PL265 can be used in non-addictive chronic pain research.

Ataquimast is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast can be used in the study of advanced receptor-positive breast cancer.

CGS 23885 is an orally active 5-lipoxygenase (5-lipoxygenase) inhibitor. CGS 23885 reduces the production of 5-hydroxyeicosatetraenoic acid (5-hydroxyeicosatetraenoic acid), LTB₄, and LTC₄/D₄/E₄. CGS 23885 inhibits cell infiltration in rat pleurisy. CGS 23885 can be used in pleurisy-related research.

LY256548 (LY25648) is an orally available anti-ischemic and anti-inflammatory compound with central nervous system activity. LY256548 is an inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and COX, and inhibits A23187 (HY-N6687)-stimulated leukotriene B4 production. LY256548 inhibits bone damage and paw swelling in the rat Freund's complete adjuvant-induced arthritis (FCA) model.

LY 245769, a omega-trifluoro analog, is a leukotriene E4 (LTE4) inhibitor. LY 245769 interfers the omega-oxidation of N-acetyl-LTE4 and leukotriene B4 (LTB4) with IC₅₀s of 4 μM.

LY329146, a Raloxifene (HY-13738) analog, is multidrug resistance protein (MRP1) inhibitor. LY329146 inhibits leucotriene C4 ( LTC4) transport with an IC₅₀ of 0.8 μM.

ONO 2050297 (Compound 19) is a selective Cysteinyl leukotriene (CysLT) antagonist with IC₅₀s of 17  and 0.87 nM for CysLT1 and CysLT2, respectively. ONO 2050297 can be used for bronchial asthma research.

L-652343 is a dual cyclooxygenase/lipoxygenase inhibitor. L-652343 can inhibit the production of LTB₄ in isolated human polymorphonuclear leukocytes treated with Calcimycin (HY-N6687) (IC₅₀: 1.4 μM), but it is inactive in whole blood. L-652343 can be used in the research of inflammatory and immune diseases.

5-LOX-IN-6 (compound 11a) is a direct and reversible inhibitor of 5-lipoxygenase (5-LO). 5-LOX-IN-6 inhibits 5-LO activity in human neutrophils and recombinant human 5-LO with IC₅₀ values of 0.23 and 0.086 µM, respectively. 5-LOX-IN-6 prevents leukotriene biosynthesis. 5-LOX-IN-6 can be used for inflammatory and allergic disorders research.

5-O-Demethylnobiletin (Standard) is the analytical standard of 5-O-Demethylnobiletin. This product is intended for research and analytical applications. 5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., is a direct inhibition of 5-LOX (IC₅₀=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC₅₀ of 0.35 μM.

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.