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-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-N16543
    Bisisorhapontigenin A
    		Antagonist
    Bisisorhapontigenin A is a dimer of isorhapontigenin. Bisisorhapontigenin A exhibits antagonistic activity against LTD4 and can be used for research on anti-inflammatory effects.
    Bisisorhapontigenin A
  • 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
  • HY-119055
    Sch 33303
    		Inhibitor
    Sch 33303 is an orally active antiallergy agent that inhibits the release of the sulfidopeptide leukotrienes. Sch 33303 is promising for research of asthma.
    Sch 33303
  • HY-168484
    T-10430
    		Agonist
    T-10430 is a potent and orally active leukotriene B4 receptor 2 (BLT2) agonist. T-10430 has the potential for the research of psoriasis.
    T-10430
  • HY-W747565
    Leukotriene B4-3-aminopropylamide
    Leukotriene B4-3-aminopropylamide (LTB4-APA) is a leukotriene immunomodulator.
    Leukotriene B4-3-aminopropylamide
  • HY-19042
    YM-16638
    		Antagonist
    YM-16638 is an orally active leukotriene (LT) antagonist. YM-16638 can inhibit the production of LTC4, LTD4, and LTE4 in guinea pig trachea, with IC50 values of 0.05 μM, 0.16 μM, and 0.096 μM, respectively. YM-16638 has a dose-dependent inhibitory effect on antigen-induced early and late respiratory responses in allergic sheep.
    YM-16638
  • HY-136831
    SR2640
    		Antagonist
    SR2640 is a highly efficient and selective LTD4/LTE4 antagonist that can specifically inhibit the smooth muscle contractions induced by LTD4 in the guinea pig ileum and trachea in a concentration-dependent manner, without affecting the contractions caused by histamine. SR2640 can concentration-dependently prevent the binding of 0.4 nM [3H] LTD4 to membrane receptors in guinea pig lung tissue, with an IC50 of 23 nM. SR2640 can shift the dose-response curve for bronchoconstriction induced by intravenous LTD4 in guinea pigs to the right, and the extent of this shift is positively correlated with the dose of SR2640 administered. SR2640 can be used in asthma research.
    SR2640
  • HY-115390
    14,15-Dehydro Leukotriene B4
    		Antagonist
    14,15-Dehydro Leukotriene B4 (Compound 4) is a LTB4 receptor antagonist. 14,15-Dehydro Leukotriene B4 also has a higher binding affinity for BLT1 with a Ki value of 27 nM and BLT2 with a Ki value of 473 nM. 14,15-Dehydro Leukotriene B4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC50 value of 1 µM.
    14,15-Dehydro Leukotriene B4
  • HY-107611
    Ro 24-5913
    		Antagonist
    Ro 24-5913 (Cinalukast) is an orally active and potent LTD4 antagonist with an IC50 value of 6.4 nM. Ro 24-5913 can be used for the research of asthma.
    Ro 24-5913
  • HY-19395
    MEN-91507
    		Antagonist
    MEN-91507 is an orally activecysteinyl leukotriene receptor 1 (CysLTR1) receptor antagonist. MEN-91507 behaves as insurmountable antagonist of Leukotriene D4 (HY-113456)-induced calcium transients, with a pKb of 10.25. MEN-91507 can inhibit Leukotriene D4-induced bronchoconstriction and microvascular leakage in guinea-pigs. MEN-91507 can be used for the researches of inflammation, immunology.
    MEN-91507
  • HY-17492S1
    Zafirlukast-13C,d3
    		Antagonist
    Zafirlukast-13C,d3 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>3</sub>
  • HY-117943
    (rac)-ONO 2050297
    		Antagonist
    (rac)-ONO 2050297 is a benzoxazole derivative and a potent biCysLT1/CysLT2 antagonist with IC50 values are 17 nM and 0.87 nM respectively.
    (rac)-ONO 2050297
  • HY-180363
    E 6080
    		Inhibitor
    E 6080 is an orally active and selective 5-lipoxygenase (5-LOX) inhibitor with an IC50 of 0.2 μM in rat basophilic leukemia cell. E 6080 shows potent inhibitory effects on the release of leukotrienes. E 6080 inhibits the bronchospasm induced by antigen (ovalbumin) inhalation in sensitized conscious guinea pigs. E 6080 can be used for the study of asthma.
    E 6080
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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