2. Signaling Pathways
  3. GPCR/G Protein
  4. Leukotriene Receptor
  5. LTE4 Isoform

LTE4

The leukotriene E4 (LTE4) receptor, now widely recognized as GPR99/OXGR1 and also referred to as CysLT3, is a G protein-coupled receptor that mediates cellular responses to the cysteinyl leukotriene LTE4, a bioactive lipid mediator involved in allergic and inflammatory reactions[1][2]. Mechanistically, LTE4-GPR99 signaling activates predominantly Gq-dependent pathways and can additionally engage Gi signaling, thereby regulating inflammatory responses in epithelial and immune cell populations[2]. The receptor participates in key biological processes associated with type 2 inflammation, bronchoconstriction, eosinophil recruitment, vascular permeability, and airway mucosal responses, linking LTE4 signaling to asthma and other allergic diseases[2][3][4]. Disease relevance is supported by observations that LTE4 levels increase in severe asthma and aspirin-exacerbated respiratory disease, while GPR99 expression in respiratory tissues contributes to inflammatory amplification[2]. Compared with the related cysteinyl leukotriene receptors CysLT1 and CysLT2, which preferentially recognize LTC4 and LTD4, GPR99 displays a distinct functional preference for LTE4 and exhibits substantial sequence divergence, supporting its classification as a separate receptor subtype within the cysteinyl leukotriene receptor family[1][2][5]. For experimental applications, GPR99 serves as a useful model for investigating LTE4-specific inflammatory signaling and for evaluating receptor-targeted therapeutic strategies in allergic disease research[1][3].

LTE4 Related Products (7):

Cat. No. Product Name Effect Purity
  • HY-19989
    MK-571
    		Antagonist 98.85%
    MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
  • HY-19989A
    MK-571 sodium
    		Antagonist 99.75%
    MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 sodium is also a inhibitor of multidrug resistance-associated protein MRP4 (ABCC4) and ABCC1 (MRP1). MK-571 sodium inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release.
  • HY-B0290
    Pranlukast
    		Antagonist 99.61%
    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.
  • 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.
  • 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.
  • 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.
  • HY-105483
    MDL 43291
    		Antagonist
    MDL 43291 is a competitive leukotriene (LT) receptor antagonist. MDL 43291 antagonize LTD4 and LTE4 with pA2 of 6.7. MDL 43291 does not antagonize histamine, carbachol or substance P. MDL 43291 can be used for the researches of inflammation and immunology, such as asthma.