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-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-15874
    Fiboflapon
    		Inhibitor 99.50%
    Fiboflapon (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
  • HY-15744
    LY255283
    		Antagonist 98.52%
    LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes.
    LY255283
  • HY-13628
    Etalocib
    		Antagonist 98.74%
    Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.
    Etalocib
  • HY-16780
    Gemilukast
    		Antagonist 99.49%
    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.
    Gemilukast
  • 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-112737
    LY223982
    		Inhibitor 99.65%
    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-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-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-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-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-108693
    β-Tocotrienol
    		98.89%
    β-Tocotrienol is one form of vitamin E. β-Tocotrienol is a less potent antioxidant than α-tocotrienol.
    β-Tocotrienol
  • 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-N1942
    5-O-Demethylnobiletin
    		Inhibitor 99.91%
    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-U00027
    Quinotolast sodium
    		Inhibitor 98.38%
    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-101438A
    Darbufelone mesylate
    		Inhibitor 99.65%
    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-111212
    Tomelukast
    		Antagonist ≥99.0%
    Tomelukast (LY171883) is an orally active leukotriene D4 and E4 antagonist. Tomelukast can be used for the research of asthma.
    Tomelukast
  • HY-15874A
    Fiboflapon sodium
    		Inhibitor 99.46%
    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-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-106929
    Moxilubant
    		Antagonist 99.83%
    Moxilubant (CGS-25019C;LTB-019) is an orally active BLT1 antagonist which inhibits LTB4 signaling with a potency of 2–4 nM. Moxilubant can be used for cancer research.
    Moxilubant
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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