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-169949
    TAK-756
    		Inhibitor
    TAK-756 is a selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with a target pIC50 of 8.6. TAK-756 can inhibit TAK1 autophosphorylation and downstream NF-κB phosphorylation, suppress the production of inflammatory and catabolic factors such as MMP-3 and IL-6. TAK-756 exhibits anti-inflammatory effects in a rat joint inflammation model. TAK-756 can be used for the research of inflammatory joint disease, osteoarthritis.
    TAK-756
  • HY-U00252
    ONO4057
    		Antagonist 99.9%
    ONO4057 is a Leukotriene B4 receptor antagonist, with an IC50 of 0.7±0.3 μM.
    ONO4057
  • HY-101946
    AS-35
    		Antagonist
    AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
    AS-35
  • HY-N4267
    Yangambin
    		Inhibitor 98.27%
    Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases.
    Yangambin
  • HY-101438A
    Darbufelone mesylate
    		Inhibitor 99.65%
    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
    Darbufelone mesylate
  • HY-112532
    REV 5901
    		Antagonist 99.9%
    REV 5901 is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 is also a 5-lipoxygenase inhibitor. REV 5901 can be used for the research of asthma in which leukotriene release be involved. REV 5901 can be used for the study of colon carcinoma.
    REV 5901
  • 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-107607
    FPL-55712 free base
    		Antagonist 98.0%
    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-120571
    L-674573
    		Inhibitor 99.54%
    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.
    L-674573
  • HY-106785
    Pobilukast
    		Antagonist 99.84%
    Pobilukast is a classical CysLT1 receptor antagonist. Pobilukast can be used for the research of asthma.
    Pobilukast
  • HY-119442
    Quininib
    		Antagonist 98.1%
    Quininib is a cysteinyl leukotriene 1 and 2 receptor antagonist with IC50s of 1.2 and 52 μM for CysLT1R and CysLT2R, respectively. Quininib is a potent inhibitor of developmental angiogenesis in the zebrafish eye. Quininib can be used for the research of ocular neovascular pathologies and may complement current anti-VEGF biological agents.
    Quininib
  • HY-17492R
    Zafirlukast (Standard)
    		Antagonist
    Zafirlukast (Standard) is the analytical standard of Zafirlukast. This product is intended for research and analytical applications. Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
    Zafirlukast (Standard)
  • HY-13315AR
    Montelukast (Standard)
    		Antagonist
    Montelukast (Standard) is the analytical standard of Montelukast. This product is intended for research and analytical applications. Montelukast (MK0476 free base) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research.
    Montelukast (Standard)
  • 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 99.60%
    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-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-135336AS1
    (S)-Verapamil-d6 (hydrochloride)
    (S)-Verapamil-d6 ((S)-(-)-Verapamil-d6) hydrochloride is the 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>6</sub> (hydrochloride)
  • 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-139112
    Leukotriene B4 dimethyl amide
    Leukotriene B4 dimethyl amide, an immunomodulator, stimulates contraction of isolated guinea pig lung entities. Leukotriene B4 (LTB(4)) also stimulates human neutrophil migration, and LTB(4) antagonists may have anti-inflammatory activity in inflammatory pathophysiology.
    Leukotriene B4 dimethyl amide
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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