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-13628
    Etalocib
    		Antagonist 99.03%
    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-13448
    Nedocromil
    		Inhibitor 98.75%
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
    Nedocromil
  • 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-114641A
    BIIL-260 hydrochloride
    		Antagonist 99.90%
    BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM.
    BIIL-260 hydrochloride
  • 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-105484
    U-75302
    		Inhibitor 99.9%
    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-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-111806
    3,7,4'-Trihydroxyflavone
    		Inhibitor 99.11%
    3,7,4'-Trihydroxyflavone (5-Deoxykampferol) is a flavonoid compound that can be isolated from the stems of Rhus javanica var. roxburghiana. 3,7,4'-Trihydroxyflavone has the effect of cleaving DNA in the presence of copper ions. 3,7,4'-Trihydroxyflavone also has anti-inflammatory and antioxidant activities and can scavenge various reactive oxygen species (ROS) and reactive nitrogen species (RNS).
    3,7,4'-Trihydroxyflavone
  • 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-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-19304
    Amelubant
    		Antagonist 98.45%
    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-107608S
    Leukotriene B4-d4
    		99.14%
    Leukotriene B4-d4 is the deuterium labeled Leukotriene B4. Leukotriene B4 (LTB4) is known as one of the most potent chemoattractants and activators of leukocytes and is involved in inflammatory diseases. Leukotriene B4 is also an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
    Leukotriene B4-d<sub>4</sub>
  • HY-106929
    Moxilubant
    		Antagonist 99.83%
    Moxilubant (CGS 25019C free base) is an orally active BLT1 antagonist. Moxilubant inhibits LTB4 signaling with a potency of 2-4 nM. Moxilubant blocks LTB4-induced neutrophil functions. Moxilubant inhibits ear edema and neutrophil infiltration in mice. Moxilubant can be used in research related to chronic obstructive pulmonary disease.
    Moxilubant
  • HY-15874A
    Fiboflapon sodium
    		Inhibitor 98.51%
    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-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-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-14165
    Veliflapon
    		Inhibitor 99.31%
    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-113483
    20-Carboxy-Leukotriene B4
    		Inhibitor 98.53%
    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-B0290R
    Pranlukast (Standard)
    		Antagonist
    Pranlukast (Standard) is the analytical standard of Pranlukast. This product is intended for research and analytical applications. 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.
    Pranlukast (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
Leukotriene Receptor Isoform Comparison

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