LTB₄ Inhibitor

Fiboflapon (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC₅₀ of 76 nM for inhibition of LTB4 in human blood.

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.

3,7,4'-Trihydroxyflavone (5-Deoxykampferol) is a flavonoid compound that can be isolated from the stems of Rhus javanica var. roxburghiana. 3,7,4'-Trihydroxyflavone has the effect of cleaving DNA in the presence of copper ions. 3,7,4'-Trihydroxyflavone also has anti-inflammatory and antioxidant activities and can scavenge various reactive oxygen species (ROS) and reactive nitrogen species (RNS).

LY223982 is a potent and specific inhibitor of leukotriene B4 receptor, with an IC₅₀ of 13.2 nM against [³H]LTB4 binding to LTB4 receptor.

Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC₅₀ of 76 nM for inhibition of LTB4 in human blood.

20-Carboxy-Leukotriene B4 (20-COOH LTB4) is a metabolite of Leukotriene B4 (LTB4; HY-107608). 20-Carboxy-Leukotriene B4 binds to the BLT1 receptor with high affinity. 20-Carboxy-Leukotriene B4 inhibits LTB4-mediated neutrophil responses (migration, degranulation, leukotriene biosynthesis).

Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

Halometasone is a corticosteroid compound that can reduce the expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP). Halometasone can be used in research on psoriasis and eczematous skin diseases.

Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC₅₀ of 29.7 μM and a K_i of 17.1 μM against human UGT1A1, and an IC₅₀ of 56.5 μM and a K_i of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB₄-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca²⁺ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases.

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).

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.

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.

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.

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.

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.

Tremulacin is a 5-LOX inhibitor. Tremulacin reduces the biosynthesis of LTB₄ and slow-reacting substances of anaphylaxis. Tremulacin alleviates carrageenan-induced paw edema in rats, croton oil-induced ear edema in mice, and acetic acid-induced writhing response in mice. Tremulacin inhibits TNF-α-stimulated ROS production and MMP-1 expression, and promotes collagen secretion in human dermal fibroblasts. Tremulacin is investigated for studies on inflammation-related diseases.

Bunaprolast (U66858) is a potent inhibitor of LTB₄ production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB₂ release.

LTB4-IN-1 (Compound 6) is a leukotriene synthesis (LTB4) inhibitor with an IC₅₀ of 70 nM.