Leukotriene Receptor Inhibitor

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.

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.

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).

(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.

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.

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.

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.

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.

(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.