1. Signaling Pathways
  2. GPCR/G Protein
  3. Leukotriene Receptor

Leukotriene Receptor

Leukotriene Receptor (cys-LTs) are a family of potent bioactive lipids that act through two structurally divergent G protein-coupled receptors, termed the CysLT1 and CysLT2 receptors. The cysteinyl leukotrienes LTC4, LTD4, and LTE4 are important mediators of human bronchial asthma. Leukotriene Receptor is a member of the superfamily of G protein-coupled receptors and uses a phosphatidylinositol-calcium second messenger system. Activation of CysLT1 by LTD4 results in contraction and proliferation of smooth muscle, oedema, eosinophil migration and damage to the mucus layer in the lung. Leukotriene receptor antagonists, called LTRAs for short, are a class of oral medication that is non-steroidal. They may also be referred to as anti-inflammatory bronchoconstriction preventors. LTRAs work by blocking a chemical reaction that can lead to inflammation in the airways.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-17492S2
    Zafirlukast-13C,d6
    Antagonist
    Zafirlukast-13C,d6 is the 13C- and deuterium labeled Zafirlukast. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
    Zafirlukast-<sup>13</sup>C,d<sub>6</sub>
  • HY-135288
    L-649923
    Antagonist
    L-649923 is an orally active CysLT1 antagonist. L-649923 reduced the incidence of gastritis in an animal model of acute gastric mucosal injury. L-649923 can be used in research on diseases such as asthma and gastritis.
    L-649923
  • HY-120539
    Enofelast
    Inhibitor
    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.
    Enofelast
  • HY-106064A
    Piriprost potassium
    Inhibitor
    Piriprost (U-60,257B) potassium is an inhibitor of leukotriene synthesis. Piriprost potassium inhibits the release of both leukotriene and histamine with an IC50 of 0.11 μM from isolated porcine lung cells. Piriprost potassium increases alkaline phosphatase (ALP) activity in cultured endometrial stromal cells.
    Piriprost potassium
  • HY-123014
    (Rac)-SC-45694
    Agonist
    (Rac)-SC-45694 is a racemate of SC-45694. SC-45694 has full LTB4 agonist activity for neutrophil chemotaxis and has antagonist activity against LTB4-induced neutrophil degranulation.
    (Rac)-SC-45694
  • HY-138050
    Nyasol
    Inhibitor
    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.
    Nyasol
  • HY-19075
    DS 4574
    Antagonist
    DS 4574 is an orally active peptidoleukotriene receptor antagonist and mast cell stabilizer. DS 4574 has antiulcer, gastroprotective and antisecretory effects. DS 4574 inhibits various types of experimental asthma models. DS 4574 protects rats from endotoxin-induced intestinal injury.
    DS 4574
  • HY-164650
    Pirodomast
    Inhibitor
    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.
    Pirodomast
  • HY-112532A
    REV 5901 hydrochloride
    Antagonist
    REV 5901 hydrochloride is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 hydrochloride is also a 5-lipoxygenase inhibitor. REV 5901 hydrochloride can be used for the research of asthma in which leukotriene release be involved. REV 5901 hydrochloride can be used for the study of colon carcinoma.
    REV 5901 hydrochloride
  • HY-124852
    ZPL-5212372
    Inhibitor
    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.
    ZPL-5212372
  • HY-19198
    SB-201993
    Antagonist
    SB-201993 is a selective leukotriene B₄ (LTB4) receptor antagonist with a Ki=7.6 nM for LTB4 receptors on human inflammatory cells. SB-201993 inhibits calcium mobilization in inflammatory cells and 5-lipoxygenase activity, exerting anti-inflammatory effects. SB-201993 is promising for research of inflammatory diseases (e.g., dermatitis, arthritis).
    SB-201993
  • HY-130138
    (5S,6S)-DiHETE
    (5S,6S)-DiHETE is an enantiomer of (5,6)-DiHETEs.
    (5S,6S)-DiHETE
  • HY-115500
    PL265
    Inhibitor
    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.
    PL265
  • HY-108162A
    Ataquimast
    Inhibitor
    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.
    Ataquimast
  • HY-117896
    SC-50605
    Antagonist
    SC-50605 and SC-51146 are second-generation leukotriene B4 (LTB4) receptor antagonists that effectively inhibit LTB4-induced chemotaxis in guinea pigs. SC-50605 targets the LTB4 receptor and has the potential to inhibit inflammatory diseases such as asthma, rheumatoid arthritis, and skin diseases..
    SC-50605
  • HY-13628A
    Etalocib sodium
    Antagonist
    Etalocib (LY293111) sodium, an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib sodium prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib sodium induces apoptosis.
    Etalocib sodium
  • HY-130138A
    (5S,6R)-DiHETE
    Activator
    (5S,6R)-DiHETE is an enantiomer of (5,6)-DiHETEs. (5S,6R)-DiHETE can be recognized by leukotriene receptors (LTD4 receptors). (5S,6R)-DiHETE can induce guinea pig isolated ileum contraction with an EC50 of 1.3 μM, and this effect can be inhibited by LTD4 receptor antagonists.
    (5S,6R)-DiHETE
  • HY-120172
    WAY-126299A
    Antagonist
    WAY-126299A is an orally active dual-acting 5-1ipoxygenase inhibitor (IC50: 12.2 μM) and leukotriene D4 antagonist (pKB: 6.4). WAY-126299A inhibits antigen-induced leukotriene-dependent bronchoconstriction. WAY-126299A can be used for research of asthma.
    WAY-126299A
  • HY-114641
    BIIL-260
    Antagonist
    BIIL-260 is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with the Ki value of 1.7 nM.
    BIIL-260
  • HY-114873
    LY256548
    Inhibitor
    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.
    LY256548
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