Leukotriene Receptor Inhibitor

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.

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.

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.

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.

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.

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.

(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.

Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C₄ (LTC₄), and prostaglandin D₂ (PGD₂).

U-75302 is a potent inhibitor of leukotriene B4. U-75302 is a pyridine analogue. U-75302 has the potential for the research of inflammatory diseases.

1-Heptanol (n-Heptyl alcohol) is a linear primary fatty alcohol. 1-Heptanol selectively inhibits the activating phosphorylation of SAPK/JNK and reduces the phosphorylation level of IκB-α. 1-Heptanol increases plasma membrane fluidity, decreases membrane thermal stability, alters the coupling kinetics of STIM1-ORAI1, inhibits the production of ROS and LTC₄, and induces the expression of HSP70. 1-Heptanol is used in the fragrance industry due to its pleasant odor.

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.

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.

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).

Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC₄ and PGD₂ release in a concentration-dependent manner.

Darbufelone 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).

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.

11(Z),14(Z)-Eicosadienoic acid is a unsaturated fattly acid that inhibits [³H] leukotriene B₄ (LTB₄) binding to pig neutrophil membranes with a K_i of 3 μM. 11(Z),14(Z)-Eicosadienoic acid has inflammatory activities.

(S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC₅₀ values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood.