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-101438
    Darbufelone
    		Inhibitor ≥98.0%
    Darbufelone is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50= 0.19 μM) but is much less potent with PGHS-1 (IC50=20 μM).
    Darbufelone
  • HY-19304
    Amelubant
    		Antagonist 99.11%
    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 proagent of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity.
    Amelubant
  • HY-101676
    RG-12525
    		Antagonist 98.31%
    RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 µM.
    RG-12525
  • HY-156978
    Ritolukast
    		Antagonist 99.92%
    Ritolukast (Wy-48252) is an orally active aerosol leukotriene (LTD4/E4) receptor antagonist. Ritolukast can be used to inhibit the bronchoconstriction caused by aerosol LTD4 in guinea pigs, with an ID50 of 0.5mg/kg.
    Ritolukast
  • 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.
    Tipelukast
  • HY-16344
    Nedocromil sodium
    		Inhibitor
    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
    Nedocromil sodium
  • 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].
    Montelukast-d<sub>6</sub> sodium
  • HY-163101
    CP-96021
    		Antagonist 98.04%
    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.
    CP-96021
  • HY-U00253
    KP496
    		Antagonist 99.79%
    KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
    KP496
  • 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.
    CAY10789
  • HY-112741
    SB-209247
    		Antagonist 99.33%
    SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a Ki of 0.78 nM. SB-209247 blocks LTB4-induced Ca2+ mobilization with an IC50 of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity.
    SB-209247
  • HY-112248
    (Rac)-HAMI 3379
    		Antagonist
    (Rac)-HAMI 3379 is the racemate of HAMI 3379. HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT2) receptor antagonist.
    (Rac)-HAMI 3379
  • HY-107610
    SR2640 hydrochloride
    		Antagonist 99.60%
    SR2640 (hydrochloride) is a potent and selective competitive leukotriene D4/leukotriene E4 antagonist. SR2640 can be used for researching the role of leukotrienes in human asthma.
    SR2640 hydrochloride
  • 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.
    AS-35
  • HY-149589
    11(Z),14(Z)-Eicosadienoic acid
    		Inhibitor ≥98.0%
    11(Z),14(Z)-Eicosadienoic acid is a unsaturated fattly acid that inhibits [3H] leukotriene B4 (LTB4) binding to pig neutrophil membranes with a Ki of 3 μM. 11(Z),14(Z)-Eicosadienoic acid has inflammatory activities.
    11(Z),14(Z)-Eicosadienoic acid
  • HY-145234
    GPBAR1-IN-3
    		Antagonist
    GPBAR1-IN-3 (Compound 14) is a selective GPBAR1 agonist (EC50=0.17 μM) and a CysLT1R antagonist.
    GPBAR1-IN-3
  • HY-105221
    Masilukast
    		Antagonist
    Masilukast is an orally administered cysteinyl leukotriene D4 (LTD4) receptor antagonist with potential to research asthma.
    Masilukast
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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