1. Signaling Pathways
  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 Isoform Specific Products:

  • LTB4

  • LTC4

  • LTD4/CysLT1

  • LTE4

  • CysLT2

  • CysLT1

Leukotriene Receptor Related Products (36):

Cat. No. Product Name Effect Purity
  • HY-19989A
    MK-571 sodium salt Antagonist 99.24%
    MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
  • HY-13315
    Montelukast sodium Antagonist 99.82%
    Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist.
  • HY-17492
    Zafirlukast Antagonist 99.90%
    Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.
  • HY-B0290A
    Pranlukast hemihydrate Antagonist 99.93%
    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.
  • HY-16780
    Gemilukast Antagonist 99.58%
    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-101438
    Darbufelone Inhibitor >98.0%
    Darbufelone is a dual inhibitor of cellular PGF and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).
  • HY-114641A
    BIIL-260 hydrochloride Antagonist
    BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride 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 Ki values of 1.7 nM.
  • HY-112248
    HAMI 3379 Antagonist
    HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation.
  • HY-13448
    Nedocromil Inhibitor
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-B0290
    Pranlukast Antagonist 99.98%
    Pranlukast 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.
  • HY-112737
    LY223982 Inhibitor >99.0%
    LY223982 is a potent and specific inhibitor of leukotriene B4 receptor, with an IC50 of 13.2 nM against [3H]LTB4 binding to LTB4 receptor.
  • 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-101946
    AS-35 Antagonist
    AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
  • HY-101438A
    Darbufelone mesylate Inhibitor
    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
  • HY-100173
    DW-1350 Antagonist
    DW-1350 is a LTB4 receptor antagonist.
  • HY-135336A
    (S)-Verapamil hydrochloride Inhibitor
    (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 is good active form and has the low bioavailability.
  • HY-N1942
    5-O-Demethylnobiletin Inhibitor
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Sideritis tragoriganum, is a direct inhibition of 5-LOX (IC50=0.1 μM), without affecting the expression of COX-2. 5-O-Demethylnobiletin (5-Demethylnobiletin) has anti-inflammatory activity, inhibits leukotriene B (4)(LTB4) formation in rat neutrophils and elastase release in human neutrophils with an IC50 of 0.35 μM.
  • HY-19193
    CP-105696 Antagonist
    CP-105696 is a potent and selective Leukotriene B4 Receptor antagonist, with an IC50 of 8.42 nM.
  • HY-14165
    Veliflapon Inhibitor
    Veliflapon (BAY X 1005; DG-031) is an orally active inhibitor of the synthesis of the leukotrienes B4 and C4. Veliflapon is shown to be a selective inhibitor of the formation of 5-lipoxygenase-derived metabolites in vitro, without effects on other routes of arachidonic acid metabolism.
  • HY-19304
    Amelubant Antagonist
    Amelubant (BIIL 284) is a potent, oral and long acting LTB4 receptor antagonist, negligibly binds to LTB4 receptor, with Kis of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity.
Isoform Specific Products

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