2. Signaling Pathways
  3. GPCR/G Protein
  4. Leukotriene Receptor

Leukotriene Receptor

Leukotriene Receptor

Related Products

PDF 0.82 MB

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-P3318
    Boc-Phe-Leu-Phe-Leu-Phe
    		Antagonist 98.10%
    Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) is a N-formyl peptide receptors (FPR) inhibitor. Boc-Phe-Leu-Phe-Leu-Phe abolishes the FMLP-induced release of peptide leukotrienes. Boc-Phe-Leu-Phe-Leu-Phe inhibits the sprouting of human umbilical vein endothelial cell (HUVEC) spheroids mediated by proliferative diabetic retinopathy (PDR) vitreous and vascular endothelial growth factor (VEGF) respectively in a three-dimensional fibrin gel. Boc-Phe-Leu-Phe-Leu-Phe inhibits the anti-inflammatory and antifibrotic effects of Ac2-26 (HY-P1098). Boc-Phe-Leu-Phe-Leu-Phe can be used for the study of immunology.
    Boc-Phe-Leu-Phe-Leu-Phe
  • HY-101438
    Darbufelone
    		Inhibitor 99.49%
    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-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.
    Pranlukast hemihydrate
  • 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-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-107609
    BAY-u 9773
    		Antagonist
    BAY-u 9773 is a selective cysteinyl-leukotriene receptor antagonist. BAY-u 9773 competitively antagonizes cysteinyl-leukotriene-induced contractions at typical and atypical cysteinyl-leukotriene receptors with comparable activity. BAY-u 9773 can be used for the research of trichomoniasis.
    BAY-u 9773
  • HY-116326
    BayCysLT2
    		Antagonist
    BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC50 value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts.
    BayCysLT2
  • HY-14165A
    (S)-Veliflapon
    		Inhibitor 99.25%
    (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.
    (S)-Veliflapon
  • 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-14938
    Tipelukast
    		Antagonist 99.49%
    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.
    Montelukast-d<sub>6</sub> sodium
  • HY-163101
    CP-96021
    		Antagonist 98.04%
    CP-96021 is an orally active dual leukotriene D4 (LTD4) and platelet activating factor (PAF) receptor antagonist, featuring a guinea pig LTD4 receptor Ki of 34 nM and a rabbit PAF receptor Ki of 37 nM. CP-96021 blocks ligand binding to its target receptors, inhibits ligand-induced bronchoconstriction, and inhibits antigen-triggered airway obstructive effects. CP-96021 can be used for the research of 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 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-W341962
    Halometasone
    		Inhibitor 98.47%
    Halometasone is a corticosteroid compound that can reduce the expression of serum leukotriene B4 (LTB4) and thymic stromal lymphopoietin (TSLP). Halometasone can be used in research on psoriasis and eczematous skin diseases.
    Halometasone
  • HY-122124
    CAY10583
    		Agonist 99.9%
    CAY10583 is a potent and selective full Leukotriene B4 receptor type 2 (BLT2) agonist. CAY10583 directly promotes keratinocyte migration in vitro and accelerates wound closure in vivo. CAY10583 is a promising pharmaceutical agent for diabetic wounds.
    CAY10583
  • 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 99.41%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.