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-113628
    ABT-080
    		Inhibitor
    ABT-080 is an orally active inhibitor of leukotriene biosynthesis. ABT-080 simultaneously blocks the leukotriene pathways leading to the synthesis of LTB4 and LTC4, but does not inhibit PGH2 biosynthesis. ABT-080 can block bronchoconstriction and be used in the research of asthma and related inflammations
    ABT-080
  • HY-N11072
    Tremulacin
    		Inhibitor
    Tremulacin is a 5-LOX inhibitor. Tremulacin reduces the biosynthesis of LTB4 and slow-reacting substances of anaphylaxis. Tremulacin alleviates carrageenan-induced paw edema in rats, croton oil-induced ear edema in mice, and acetic acid-induced writhing response in mice. Tremulacin inhibits TNF-α-stimulated ROS production and MMP-1 expression, and promotes collagen secretion in human dermal fibroblasts. Tremulacin is investigated for studies on inflammation-related diseases.
    Tremulacin
  • HY-176920
    BRI-12349
    		Antagonist
    BRI-12349 (Compound 50) is a dual antagonist of CysLT1R/CysLT2R with Ki values of 1.03 and 6.46 μM. BRI-12349 can inhibit the generation of IP1 induced by LTD4 (the main ligand of CysLTs). BRI-12349 can be used for the research of immunology and inflammation, such as asthma.
    BRI-12349
  • HY-123571
    CP-199330
    		Antagonist
    CP-199330 is a potent and orally active cysteinyl LT1 receptor antagonist.
    CP-199330
  • HY-B0290AR
    Pranlukast hemihydrate (Standard)
    		Antagonist
    Pranlukast (hemihydrate) (Standard) is the analytical standard of Pranlukast (hemihydrate). This product is intended for research and analytical applications. Pranlukast hemihydrate 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 hemihydrate (Standard)
  • HY-101686
    LM-1484
    		Antagonist
    LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for 3H-LTC4 sites.
    LM-1484
  • HY-U00072
    RS-601
    		Antagonist
    RS-601 is a novel leukotriene D4 (LTD4)/thromboxane A2 (TxA2) dual receptor antagonist, with antiasthmatic activities.
    RS-601
  • HY-165155
    CysLT1 receptor antagonist-1
    		Antagonist
    CysLT1 receptor antagonist-1 (Compound 4) is an antagonist for cysteinyl leukotriene receptor 1 (CysLT1R) with an IC50 of 3.9 μM. CysLT1 receptor antagonist-1 exhibits weak agonist activity against G-protein-coupled bile acid receptor 1 (GPBAR1) with an efficact of 23% at 10 μM. CysLT1 receptor antagonist-1 can be used for asthma and allergic diseases researchs.
    CysLT1 receptor antagonist-1
  • HY-168784
    LTD4 antagonist 2
    		Antagonist
    LTD4 antagonist 2 (compound 6) is a leukotriene D4 (LTD4) antagonist with an IC50 of 2.8 μM against cysteinyl leukotriene 1 receptor (CysLT1R). LTD4 antagonist 2 is also a G protein-coupled bile acid receptor 1 (GPBAR1) agonist and can be utilized in research related to colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.
    LTD4 antagonist 2
  • HY-108693R
    β-Tocotrienol (Standard)
    β-Tocotrienol (Standard) is the analytical standard of β-Tocotrienol. This product is intended for research and analytical applications. β-Tocotrienol is an isomer of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol. β-Tocotrienol can be found in the tocotrienol-rich fraction (TRF) of palm oil, which possesses anti-carcinogenic effects in vitro on human colon carcinoma and prostate cancer cells. β-Tocotrienol inhibits the growth of A549 (GI50 = 1.38 μM) and U87MG (GI50 = 2.53 μM) cells. β-Tocotrienol also induces apoptosis in cancer cells. β-Tocotrienol can inhibit PD-L1 expression and mitigates PD-L1-mediated immune suppression in vitro and in vivo.
    β-Tocotrienol (Standard)
  • HY-105176
    Ontazolast
    		Inhibitor
    Ontazolast (BIRM 270) is a potent inhibitor of LTB4 biosynthesis. Ontazolast can be used in research on asthma.
    Ontazolast
  • HY-100316
    CP-96486
    		Antagonist
    CP-96486 is a potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Kis of 20 and 24 nM, respectively.
    CP-96486
  • 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.
    Verlukast-d<sub>6</sub>
  • HY-108963
    LY 170198
    		Antagonist
    LY 170198 is a protein kinase C inhibitor and a LTD4 antagonist. LY 170198 is promising for research of tumor promotion, oncogene activation, protein phosphorylation, feedback mechanisms in signal transduction and cellular responses to growth factors.
    LY 170198
  • HY-107610R
    SR2640 hydrochloride (Standard)
    		Antagonist
    SR2640 hydrochloride (Standard) is the analytical standard of SR2640 (hydrochloride) (HY-107610). This product is intended for research and analytical applications. SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma.
    SR2640 hydrochloride (Standard)
  • HY-U00359
    LTD4 antagonist 1
    		Antagonist
    LTD4 antagonist 1 is a potent, orally active antagonist of leukotriene D4 (LTD4) with a Ki of 0.57 nM.
    LTD4 antagonist 1
  • HY-U00263
    LY210073
    		Antagonist
    LY210073 is a Leukotriene B4 (LTB4) receptor antagonist with an IC50 of 6.2 nM.
    LY210073
  • HY-U00364
    CI-949
    		Inhibitor
    CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C4/D4 (LTC4/LTD4), and thromboxane B2 (TXB2) release with IC50s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.
    CI-949
  • HY-U00355
    YM158 free base
    		Antagonist
    YM158 free base is a potent and selective LTD4 and TXA2 receptor antagonist with pA2 values of about 8.87 and 8.81, respectively.
    YM158 free base
  • HY-U00170
    Bunaprolast
    		Inhibitor
    Bunaprolast (U66858) is a potent inhibitor of LTB4 production in human whole blood. Bunaprolast (U66858) also exhibits significant inhibition of lipoxygenase and TXB2 release.
    Bunaprolast
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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