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-14938
    Tipelukast
    		Antagonist ≥99.0%
    Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
    Tipelukast
  • HY-145234
    GPBAR1-IN-3
    		Antagonist
    GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and a CysLT1R antagonist.
    GPBAR1-IN-3
  • HY-105221
    Masilukast
    		Antagonist
    Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to research asthma.
    Masilukast
  • HY-14166A
    MK-886 sodium salt
    		Inhibitor
    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.
    MK-886 sodium salt
  • HY-19989
    MK-571
    		Antagonist
    MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
    MK-571
  • HY-13315B
    Montelukast dicyclohexylamine
    		Antagonist
    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
  • HY-130440
    Leukotriene F4
    Leukotriene F4 (LTF4), is a lipid that belongs to the Cysteinyl Leukotriene (CysTL) family. Leukotriene F4 induces bronchoconstriction with an ED50 of 16 μg/kg. The precursor of LTF4 is Leukotriene E4 (LTE4), which isformed from the action of a glutamyl transferase.
    Leukotriene F4
  • HY-111212
    Tomelukast
    		Antagonist
    Tomelukast (LY171883) is an orally active leukotriene D4 and E4 antagonist. Tomelukast can be used for the research of asthma.
    Tomelukast
  • 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-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-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-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[1].
    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-147086
    CAY10789
    		Antagonist 99.84%
    CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.
    CAY10789
  • 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-107608S
    Leukotriene B4-d4
    Leukotriene B4-d4 is the deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1][2][3].
    Leukotriene B4-d<sub>4</sub>
  • 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
Leukotriene Receptor Isoform Comparison

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