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-14165
    Veliflapon
    		Inhibitor 99.48%
    Veliflapon (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor. Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.
    Veliflapon
  • HY-N1942
    5-O-Demethylnobiletin
    		Inhibitor 99.93%
    5-O-Demethylnobiletin (5-Demethylnobiletin), a polymethoxyflavone isolated from Citrus jambhiri Lush., 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.
    5-O-Demethylnobiletin
  • 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-B0174A
    Olsalazine
    		Inhibitor 99.64%
    Olsalazine is a potent inhibitor of macrophages chemotaxis to LTB4 with an IC50 value of 0.39 mM, also reduces the synthesis of 5-hydroxyeicosatetraenoic acid (5-HETE), 11-HETE, 12-HETE, and 15-HETE in polymorphonuclear leukocyte (PMNL) and mononuclear cells (MNL). Olsalazine can be used for researching ulcerative colitis. Anti-inflammatory activity.
    Olsalazine
  • HY-113330
    12S-HHT
    		Agonist ≥99.0%
    12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H2 (PGH2) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenous ligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity.
    12S-HHT
  • 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.
    Fiboflapon sodium
  • HY-112737
    LY223982
    		Inhibitor 99.67%
    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.
    LY223982
  • HY-101438A
    Darbufelone mesylate
    		Inhibitor 98.45%
    Darbufelone mesylate (CI-1004 mesylate) 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 mesylate
  • HY-105484
    U-75302
    		Inhibitor ≥99.0%
    U-75302 is a potent inhibitor of leukotriene B4. U-75302 is a pyridine analogue. U-75302 has the potential for the research of inflammatory diseases.
    U-75302
  • HY-76511
    Verlukast
    		98.61%
    Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma.
    Verlukast
  • HY-135336A
    (S)-Verapamil hydrochloride
    		Inhibitor 98.30%
    (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
  • HY-U00253
    KP496
    		Antagonist 99.79%
    KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.
    KP496
  • HY-112248A
    HAMI 3379
    		Antagonist 99.76%
    HAMI 3379 is a potent and selective CysLT2 receptor antagonist. HAMI 3379 has a protective effect on acute and subacute ischemic brain injury, and attenuates microglia-related inflammation.
    HAMI 3379
  • HY-108396
    γ-Linolenic acid ethyl ester
    		Antagonist 99.14%
    γ-Linolenic acid ethyl ester (Ethyl γ-linolenate) is a leukotriene B4 receptor 4 (LTB4) antagonist.
    γ-Linolenic acid ethyl ester
  • HY-113483
    20-Carboxy-Leukotriene B4
    		Inhibitor ≥98.0%
    20-Carboxy-Leukotriene B4 (20-COOH LTB4) is a metabolite of Leukotriene B4 (LTB4; HY-107608). 20-Carboxy-Leukotriene B4 binds to the BLT1 receptor with high affinity. 20-Carboxy-Leukotriene B4 inhibits LTB4-mediated neutrophil responses (migration, degranulation, leukotriene biosynthesis).
    20-Carboxy-Leukotriene B4
  • HY-U00027
    Quinotolast sodium
    		Inhibitor 98.12%
    Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
    Quinotolast sodium
  • 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-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-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
Leukotriene Receptor Isoform Comparison

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