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

Leukotriene Receptor

Leukotriene Receptor

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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.

Leukotriene Receptor Isoform Specific Products:

Leukotriene Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-130138B
    (5S,6R)-DiHETEs
    		Control
    (5S,6R)-DiHETEs is the isomer of (5S,6R)-DiHETE (HY-130138A). (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)-DiHETEs
  • HY-155204
    LTB4-IN-2
    		Inhibitor
    LTB4-IN-2 (Comopund 6x) is a Leukotriene B4 (LTB4) inhibitor. LTB4-IN-2 inhibits Leukotriene B4 formation (IC50: 1.15 μM) by selectively targeting 5-Lipoxygenase-activating protein (FLAP). LTB4-IN-2 can be used for anti-inflammatory research.
    LTB4-IN-2
  • HY-100724
    YM-17690
    		Agonist
    YM-17690 is a LTD4 and LTE4 agonist, with a pKi value of 9.28 for [3H]LTD4. It induces dose-dependent contractions in guinea pig ileum, lung parenchyma, and trachea, with EC50 values of 16, 3.9, and 22 nM, respectively. YM-17690 can be used in research related to asthma and inflammation.
    YM-17690
  • HY-N6607R
    Tryptanthrin (Standard)
    		Inhibitor
    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.
    Tryptanthrin (Standard)
  • HY-112736
    RG 14893
    		Antagonist
    RG 14893 is a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
    RG 14893
  • HY-107607
    FPL-55712 free base
    		Antagonist
    FPL-55712 free base is a leukotriene receptor antagonist. FPL-55712 free base is also an antagonist of slow reacting substance of anaphylaxis (SRS-A). FPL-55712 free base inhibits leukotriene-induced bronchoconstriction.
    FPL-55712 free base
  • HY-116326
    BayCysLT2
    		Antagonist
    BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts.
    BayCysLT2
  • HY-120571
    L-674573
    		Inhibitor 99.54%
    L-674573 is a quinoline leukotriene synthesis inhibitor that selectively inhibits 5-lipoxygenase translocation.
    L-674573
  • HY-118958
    Ablukast
    		Antagonist 99.36%
    Ablukast (Ro 23-3544) is a specific and active leukotriene receptor antagonist. Ablukast effectively reduces LTC4- and antigen-induced bronchoconstriction. Ablukast is LTD4 receptor antagonist.
    Ablukast
  • HY-106785
    Pobilukast
    		Antagonist
    Pobilukast is a classical CysLT1 receptor antagonist. Pobilukast can be used for the research of asthma.
    Pobilukast
  • HY-76511S
    Verlukast-d6
    		Antagonist
    Verlukast-d6 is a deuterium labeled Verlukast. Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
    Verlukast-d<sub>6</sub>
  • HY-14165A
    (S)-Veliflapon
    		Inhibitor 99.44%
    (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.
    (S)-Veliflapon
  • HY-B0290S1
    Pranlukast-d4
    		Antagonist
    Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.
    Pranlukast-d<sub>4</sub>
  • HY-118979
    L-691678
    		Inhibitor
    L-691678 can bind to FLAP by recognizing the amino acid residues of 5-lipoxygenase-activating protein (FLAP), thereby inhibiting leukotriene biosynthesis. L-691678 can be used in the study of leukotriene-related diseases such as allergies, asthma, and inflammation.
    L-691678
  • HY-117854
    SB 201146
    		Antagonist
    SB 201146 is an LTB4 receptor antagonist with a potency range of 10 pM to 1 μM that plays a critical role in asthma-associated airway inflammation. Studies have focused on its effects on eosinophil survival, a hallmark of asthma pathology. Studies have shown that eosinophil-derived cysteinyl leukotrienes, including LTC4 and LTD4, as well as factors such as GM-CSF and fibronectin promote eosinophil survival. SB 201146 effectively reversed mast cell- and lymphocyte-induced eosinophil survival, highlighting its potential therapeutic role in disrupting the autocrine cysteinyl leukotriene pathway that maintains eosinophil viability. This antagonist also highlights the importance of LTB4 as a paracrine mediator that influences eosinophil survival in inflammatory settings such as asthma.
    SB 201146
  • HY-127113
    Q8
    		Antagonist
    Q8, an effective antiangiogenic drug, is a CysLt1 antagonist (IC50 of 4.9 μM). Q8 is sufficient to reduce cellular levels of NF-κB and calpain-2 and secreted levels of the proangiogenic proteins intercellular adhesion molecule-1, vascular cell adhesion protein-1, and VEGF.
    Q8
  • HY-120486
    LY203647
    		Antagonist
    LY203647 is an orally active antagonist for leukotriene receptor LTD4 and LTE4. LY203647 can be used in research about asthma and other inflammation diseases.
    LY203647
  • HY-19109
    RG-7152
    		Antagonist
    RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator.
    RG-7152
  • HY-13448R
    Nedocromil (Standard)
    		Inhibitor
    Nedocromil (Standard) is the analytical standard of Nedocromil. This product is intended for research and analytical applications. Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
    Nedocromil (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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