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 (78):

Cat. No. Product Name Effect Purity
  • HY-17492
    Zafirlukast Antagonist 99.90%
    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-15744
    LY255283 Antagonist
    LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes[1][2][3][4].
  • 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-149082
    LTB4 antagonist 1 Antagonist
    LTB4 antagonist 1, a carboxamide-acid compound, is a potent Leukotriene B4 (LTB4) antagonist with an IC50 of 288 nM. LTB4 antagonist 1 has significant anti-inflammatory properties[1].
  • HY-149083
    LTB4 antagonist 2 Antagonist
    LTB4 antagonist 2, a carboxamide-acid compound, is an antagonist of leukotriene B4 (LTB4) with potentially anti-inflammatory activity. LTB4 antagonist 2 shows good affinity for the LTB4 receptor with IC50 of 439 nM[1].
  • HY-14165A
    (S)-Veliflapon Inhibitor 99.44%
    (S)-Veliflapon ((S)-BAY X 1005) is an orally active inhibitor of leukotriene biosynthesis and 5-lipoxygenase activating protein (FLAP). (S)-Veliflapon inhibits the formation of leukotriene B4 (LTB4) in rat, mouse and human leukocytes with IC50 values of 0.026 µM, 0.039 µM and 0.22 µM respectively. (S)-Veliflapon showes enantioselectivity in human whole blood[1][2][3].
  • 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-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-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.
  • HY-13315S1
    Montelukast-d6 sodium Antagonist
    Montelukast-d6 (sodium) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). 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[1].
  • HY-17492S
    Zafirlukast-d7 Antagonist
    Zafirlukast-d7 is the 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[1][2].
  • HY-U00263
    LY210073 Antagonist
    LY210073 is a Leukotriene B4 (LTB4) receptor antagonist with an IC50 of 6.2 nM.
  • HY-105221
    Masilukast Antagonist
    Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to research asthma.