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-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 hydrochloride-d6
    (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 hydrochloride-d<sub>6</sub>
  • 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
  • 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-120539
    Enofelast
    		Inhibitor
    Enofelast (BI-L-239), a 5-lipoxygenase (5-LO) inhibitor, exhibits an IC50 of 2.48 μM for inhibition of calcium ionophore-induced LTB4 generation.
    Enofelast
  • 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-123014
    (Rac)-SC-45694
    		Agonist
    (Rac)-SC-45694 is a racemate of SC-45694. SC-45694 has full LTB4 agonist activity for neutrophil chemotaxis and has antagonist activity against LTB4-induced neutrophil degranulation.
    (Rac)-SC-45694
  • 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-164650
    Pirodomast
    		Inhibitor
    Pirodomast (Sch 37224) is a leukotriene formation inhibitor. Pirodomast inhibits LTD4 andthromboxane B2 release by anaphylactic guinea pig lung with the IC50 values of 3.9 and 1.9 μM, respectively. Pirodomast can be used for study of asthma.
    Pirodomast
  • HY-112532A
    REV 5901 hydrochloride
    		Antagonist
    REV 5901 hydrochloride is a competitive and orally active antagonist of leukotriene receptor, with a Ki of 0.7 μM. REV 5901 hydrochloride is also a 5-lipoxygenase inhibitor. REV 5901 hydrochloride can be used for the research of asthma in which leukotriene release be involved. REV 5901 hydrochloride can be used for the study of colon carcinoma.
    REV 5901 hydrochloride
  • HY-130138
    (5S,6S)-DiHETE
    (5S,6S)-DiHETE is an enantiomer of (5,6)-DiHETEs.
    (5S,6S)-DiHETE
  • HY-108162A
    Ataquimast
    		Inhibitor
    Ataquimast is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast can be used in the study of advanced receptor-positive breast cancer.
    Ataquimast
  • HY-117896
    SC-50605
    		Antagonist
    SC-50605 and SC-51146 are second-generation leukotriene B4 (LTB4) receptor antagonists that effectively inhibit LTB4-induced chemotaxis in guinea pigs. SC-50605 targets the LTB4 receptor and has the potential to inhibit inflammatory diseases such as asthma, rheumatoid arthritis, and skin diseases..
    SC-50605
  • HY-13628A
    Etalocib sodium
    		Antagonist
    Etalocib (LY293111) sodium, an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib sodium prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib sodium induces apoptosis.
    Etalocib sodium
  • HY-130138A
    (5S,6R)-DiHETE
    		Activator
    (5S,6R)-DiHETE is an enantiomer of (5,6)-DiHETEs. (5S,6R)-DiHETE can be recognized by leukotriene receptors (LTD4 receptors). (5S,6R)-DiHETE can induce guinea pig isolated ileum contraction with an EC50 of 1.3 μM, and this effect can be inhibited by LTD4 receptor antagonists.
    (5S,6R)-DiHETE
  • HY-114641
    BIIL-260
    		Antagonist
    BIIL-260 is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with the Ki value of 1.7 nM.
    BIIL-260
  • HY-114873
    LY256548
    		Inhibitor
    LY256548 (LY25648) is an orally available anti-ischemic and anti-inflammatory compound with central nervous system activity. LY256548 is an inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and COX, and inhibits A23187 (HY-N6687)-stimulated leukotriene B4 production. LY256548 inhibits bone damage and paw swelling in the rat Freund's complete adjuvant-induced arthritis (FCA) model.
    LY256548
  • HY-123575
    LY 245769
    		Inhibitor
    LY 245769, a omega-trifluoro analog, is a leukotriene E4 (LTE4) inhibitor. LY 245769 interfers the omega-oxidation of N-acetyl-LTE4 and leukotriene B4 (LTB4) with IC50s of 4 μM.
    LY 245769
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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