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-13315S
    Montelukast-d6
    		Antagonist
    Montelukast-d6 is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
    Montelukast-d<sub>6</sub>
  • HY-142521
    BLT2 probe 1
    BLT2 probe 1 (compound 13) is a fluorescent probe based on the synthetic BLT2 agonist CAY10583. BLT2 is a promising target for diabetic wound healing and gastrointestinal lesions. BLT2 probe 1 is suitable to investigate the pharmacology of BLT2 receptor ligands in a variety of assay systems.
    BLT2 probe 1
  • HY-113758
    LY 163443
    		Antagonist
    LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4.
    LY 163443
  • HY-P3318
    Boc-Phe-Leu-Phe-Leu-Phe
    		Antagonist 98.03%
    Boc-Phe-Leu-Phe-Leu-Phe, a chemotactic peptide antagonist, abolishes the FMLP-induced release of peptide leukotrienes.
    Boc-Phe-Leu-Phe-Leu-Phe
  • HY-120931
    LY329146
    		Inhibitor
    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.
    LY329146
  • HY-149082
    LTB4 antagonist 1
    		Antagonist
    LTB4 antagonist 1, a carboxamide-acid compound, is a potent Leukotriene B4 (LTB4) antagonist with an IC50 of 288 nM. LTB4 antagonist 1 has significant anti-inflammatory properties.
    LTB4 antagonist 1
  • HY-134123
    Lipoxin B4 methyl ester
    Lipoxin B4 (LXB4) methyl ester is a lipid soluble prodrug form of the transcellular metabolite LXB4. LXB4 is a positional isomer of LXA4 produced by the metabolism of 15-HETE or 15-HpETE by human leukocytes. At a concentration of 100 nM, LXB4 inhibits polymorphonuclear leukocyte (PMN) migration stimulated by leukotriene B4 (LTB4; Item No. 20110) and inhibits LTB4-induced adhesion of PMNs with an IC50 value of 0.3 nM.
    Lipoxin B4 methyl ester
  • HY-100173
    DW-1350
    		Antagonist
    DW-1350 is a LTB4 receptor antagonist.
    DW-1350
  • HY-120502
    5-LOX-IN-6
    		Inhibitor
    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.
    5-LOX-IN-6
  • HY-112742
    CP-195543
    		Antagonist
    CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration.
    CP-195543
  • HY-N1942R
    5-O-Demethylnobiletin (Standard)
    		Inhibitor
    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.
    5-O-Demethylnobiletin (Standard)
  • HY-134092
    N-Methyl Leukotriene C4
    		Agonist
    N-Methyl Leukotriene C4 stimulates contraction of airway smooth muscle in animals, with efficacy varying by tissue and species. For example, it can stimulate the lungs of bullfrogs to contract.
    N-Methyl Leukotriene C4
  • HY-W744275
    Tipelukast-d6
    Tipelukast-d6 is the deuterium labeled Tipelukast (HY-14938). Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
    Tipelukast-d<sub>6</sub>
  • HY-113484
    Leukotriene B5
    		Activator
    Leukotriene B5 (LTB5) is a leukotriene with diverse biological activities. It is a metabolite of eicosapentaenoic acid formed through the 5-lipoxygenase (5-LO) pathway. LTB5 increases contraction of bullfrog lung strips ex vivo in a concentration-dependent manner. In vivo, LTB5 (100 nM) reduces tumor volume in mice injected with Tm1 murine melanoma cells. LTB5 also elicits chemokinesis and lysosomal enzyme release from polymorphonuclear leukocytes (PMNLs) 20- to 30-fold less, and induces platelet aggregation 8-fold less, potently than LTB4.
    Leukotriene B5
  • HY-W747548
    12(S)-HEPE
    		Inhibitor
    12(S)-HEPE is a monohydroxy fatty acid synthesized from EPA by the action of 12-LO. Unstimulated neutrophils metabolize 12(S)-HEPE to 12(S),20-diHEPE, whereas stimulated neutrophils produce 5(S),12(S)-HEPE via the 5-lipoxygenase pathway. The competitive action of 12(S)-HEPE with arachidonic acid as a substrate for 5-LO in the formation of leukotrienes may provide a basis for the anti-inflammatory potential of ω-3 fatty acids.
    12(S)-HEPE
  • HY-156960
    JNJ-40929837
    		Inhibitor
    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.
    JNJ-40929837
  • HY-112739
    SC-41930
    		Agonist
    SC-41930 is a orally active eukotriene-B4 receptor antagonist. SC-41930 alleviates inflammation in guinea pig acetic acid-induced colonic inflammation model.
    SC-41930
  • HY-13315BR
    Montelukast dicyclohexylamine (Standard)
    		Antagonist
    Montelukast (dicyclohexylamine) (Standard) is the analytical standard of Montelukast (dicyclohexylamine). This product is intended for research and analytical applications. Montelukast (MK0476) dicyclohexylamine is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast dicyclohexylamine can be used for the reseach of asthma and liver injury. Montelukast dicyclohexylamine also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast dicyclohexylamine decreases eosinophil infiltration into the asthmatic airways. Montelukast dicyclohexylamine can also be used for COVID-19 research.
    Montelukast dicyclohexylamine (Standard)
  • HY-135336AS
    (S)-Verapamil-d7 hydrochloride
    		Inhibitor
    (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.
    (S)-Verapamil-d<sub>7</sub> hydrochloride
  • HY-155300
    BLT2 antagonist-1
    		Antagonist
    BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease.
    BLT2 antagonist-1
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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