2. GPCR/G Protein
  3. Leukotriene Receptor

Leukotriene Receptor

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 Related Products (107):

Cat. No. Product Name Effect Purity
  • HY-17492
    Zafirlukast Antagonist 99.89%
    Zafirlukast (ICI 204219) is a potent orally active leukotriene D4 (LTD4) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.
  • HY-19989A
    MK-571 sodium Antagonist
    MK-571 (L-660711) sodium 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 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].
  • HY-107608
    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].
  • HY-13315
    Montelukast sodium Antagonist 99.52%
    Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). 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. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research[1][2][3][4].
  • HY-14166
    MK-886 Inhibitor 99.77%
    MK-886 (L 663536) 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 is also a non-competitive PPARα antagonist and can induce apoptosis[1][2][3].
  • 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[1].
  • HY-B0174AS2
    Olsalazine-d3,15N Inhibitor
    Olsalazine-d3,15N is 15N and deuterated labeled Olsalazine (HY-B0174A). Olsalazine is a potent inhibitor of macrophages chemotaxis to LTB4 with an IC50 value of 0.39 mM, also reduces the synthesis of 5-hydroxyeicosatetraenoic acid (5-HETE), 11-HETE, 12-HETE, and 15-HETE in polymorphonuclear leukocyte (PMNL) and mononuclear cells (MNL). Olsalazine can be used for researching ulcerative colitis. Anti-inflammatory activity[1][2].
  • HY-W747565
    Leukotriene B4-3-aminopropylamide
    Leukotriene B4-3-aminopropylamide (LTB4-APA) is a leukotriene immunomodulator. The study found that LTB4 can bind to the polar carboxylic acid group of LTB4 near the outer surface of BLT1 cells, and the hydrophobic LTB4 tail points to the transmembrane region of the receptor protein[1].
  • HY-13448
    Nedocromil Inhibitor
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-130440
    Leukotriene F4
    Leukotriene F4 (LTF4), is a lipid that belongs to the Cysteinyl Leukotriene (CysTL) family[1]. Leukotriene F4 induces bronchoconstriction with an ED50 of 16 μg/kg[2]. The precursor of LTF4 is Leukotriene E4 (LTE4), which isformed from the action of a glutamyl transferase[1].
  • HY-16344
    Nedocromil sodium Inhibitor
    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-111212
    Tomelukast Antagonist
    Tomelukast (LY171883) is an orally active leukotriene D4 and E4 antagonist. Tomelukast can be used for the research of asthma[1].
  • 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.
  • 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.
  • HY-N6607
    Tryptanthrin Inhibitor
    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[1][2].
  • HY-15874A
    Fiboflapon sodium Inhibitor 99.91%
    Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood[1].
  • 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[1].
  • 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[1][2].
  • 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[1][2].
  • HY-16780
    Gemilukast Antagonist 99.50%
    Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively. Gemilukast is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.