2. Signaling Pathways
  3. GPCR/G Protein
  4. Leukotriene Receptor
  5. LTD4/CysLT1 Isoform
  6. LTD4/CysLT1 Antagonist

LTD4/CysLT1 Antagonist

LTD4/CysLT1 Antagonists (24):

Cat. No. Product Name Effect Purity
  • HY-19989A
    MK-571 sodium
    		Antagonist 99.24%
    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.
  • HY-13315
    Montelukast sodium
    		Antagonist 99.84%
    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.
  • 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-13315A
    Montelukast
    		Antagonist 99.94%
    Montelukast (MK0476 free base) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT1). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research.
  • HY-B0290
    Pranlukast
    		Antagonist 98.18%
    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-163101
    CP-96021
    		Antagonist
    CP-96021 is a potent and orally available leukotriene D4 (LTD4 Ki=34 μM) / platelet activating factor (PAF Ki=37 μM) receptor antagonist. CP-96021 has antagonist capable of simultaneously targeting two different inflammatory mediators, LTD4 and PAF. CP-96021 shows high specificity for α1, α2, β, dopamine-2, adenosine 1, 5-HT1, H1, muscarine, μ opioid, and GABA receptors, all expressing IC50 values greater than 10 μM. CP-96021 can be used to study the pathogenesis of many inflammatory diseases such as asthma.
  • HY-165155
    CysLT1 receptor antagonist-1
    		Antagonist
    CysLT1 receptor antagonist-1 (Compound 4) is an antagonist for cysteinyl leukotriene receptor 1 (CysLT1R) with an IC50 of 3.9 μM. CysLT1 receptor antagonist-1 exhibits weak agonist activity against G-protein-coupled bile acid receptor 1 (GPBAR1) with an efficact of 23% at 10 μM. CysLT1 receptor antagonist-1 can be used for asthma and allergic diseases researchs.
  • HY-19989
    MK-571
    		Antagonist 98.56%
    MK-571 (L-660711) 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 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
  • 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.
  • HY-B0290A
    Pranlukast hemihydrate
    		Antagonist 99.28%
    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-14938
    Tipelukast
    		Antagonist 99.40%
    Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
  • HY-U00253
    KP496
    		Antagonist 99.79%
    KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
  • HY-147086
    CAY10789
    		Antagonist 99.84%
    CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.
  • 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-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.
  • HY-N8892
    Triptinin B
    		Antagonist
    Triptinin B (compound 2) is a LTD4 antagonist that can be isolated from Tripterygium wilfordii.
  • HY-107609
    BAY-u 9773
    		Antagonist
    BAY-u 9773 is a non-selective antagonist of the CysLT receptors (cysteinyl leukotrienes receptors) with about the same IC50 for CysLT1 and CysLT2. BAY-u9773 is used for the inhibition of LT responses.
  • HY-118958
    Ablukast
    		Antagonist 99.36%
    Ablukast (Ro 23-3544) is a specific and active leukotriene receptor antagonist. Ablukast effectively reduces LTC4- and antigen-induced bronchoconstriction. Ablukast is LTD4 receptor antagonist.
  • HY-119442
    Quininib
    		Antagonist
    Quininib is a cysteinyl leukotriene 1 and 2 receptor antagonist with IC50s of 1.2 and 52 μM for CysLT1R and CysLT2R, respectively. Quininib is a potent inhibitor of developmental angiogenesis in the zebrafish eye. Quininib can be used for the research of ocular neovascular pathologies and may complement current anti-VEGF biological agents.
  • HY-101686
    LM-1484
    		Antagonist
    LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for 3H-LTC4 sites.