2. シグナル伝達
  3. GPCR/G Protein
  4. Leukotriene Receptor
  5. LTC4/CysLT2 Isoform

LTC4/CysLT2

LTC4/CysLT2 (CYSLTR2) is a cysteinyl leukotriene signaling axis that regulates inflammatory and vascular responses through a G protein-coupled receptor predominantly coupled to Gq/11-dependent signaling pathways[3][4]. CysLT2 functions as a receptor for cysteinyl leukotrienes and contributes to leukotriene-induced modulation of smooth muscle contraction, vascular permeability, and leukocyte activation, placing this pathway at the center of allergic and inflammatory biology[3]. Mechanistically, LTC4 activates CysLT2-dependent cellular responses, including calcium signaling in endothelial cells and cytokine-associated inflammatory programs in immune cells and platelets[5][6][1]. In disease settings, CysLT2 signaling has been linked to eosinophilic type 2 immunopathology, aspirin-exacerbated respiratory disease-like inflammation, dermatitis-associated itch responses, and allergic airway disorders[1][2][7]. Compared with the closely related CysLT1 receptor, CysLT2 displays distinct pharmacological and biological properties; CysLT2 can negatively regulate CysLT1-dependent pulmonary Th2 inflammation, and several classical CysLT1 antagonists, including montelukast, show little or no activity at CysLT2[3][6]. This functional divergence is important for experimental design because receptor-selective signaling may influence inflammatory outcomes independently of CysLT1 pathways[6]. For research applications, selective CysLT2 antagonists have been reported to block vascular permeability and myocardial ischemia/reperfusion injury in experimental models, providing useful tools for mechanistic studies of leukotriene biology and inflammatory disease processes[3].

LTC4/CysLT2 関連製品 (23):

製品番号 製品名 製品効果 純度
  • HY-112248A
    HAMI 3379 Antagonist 98.64%
    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.
  • 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-135336A
    (S)-Verapamil hydrochloride Inhibitor 99.02%
    (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.
  • HY-13448
    Nedocromil Inhibitor 98.75%
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • 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.
  • HY-134092
    N-Methyl Leukotriene C4 Agonist
    N-Methyl Leukotriene C4 (N-Methyl-LTC4) is a non-metabolizable LTC4 analog and a selective cysteinyl leukotriene receptor 2 (CysLT2) agonist, with an EC50 of 46.1 nM for mouse CysLT2 and an EC50 value of 122.3 nM for human CysLT2. N-Methyl Leukotriene C4 shows low potency against CysLT1. N-Methyl Leukotriene C4 activates human and mouse CysLT2 receptors, triggering calcium signaling, β-arrestin-2 binding to phosphorylated receptors, vascular leakage, hypotension, tachycardia, contraction of guinea pig ileum and trachea, mild bronchoconstriction, as well as hypertension associated with peripheral vasoconstriction. N-Methyl Leukotriene C4 can be used in research on asthma, rhinitis, sinusitis, cerebral inflammation and edema, pulmonary arterial hypertension, and cardiovascular diseases.
  • HY-185709
    2-ARA-LysoPtdEtn Inhibitor
    2-ARA-LysoPtdEtn (1-Lyso-2-arachidonoyl-sn-glycero-3-phosphoethanolamine) is an orally active polyunsaturated acyl lysophosphatidylethanolamine. 2-ARA-LysoPtdEtn diminishes formation of LTC4, LTB4, and 12-HETE. 2-ARA-LysoPtdEtn lowers levels of IL-1β, IL-6, TNF-α, and NO. 2-ARA-LysoPtdEtn augments IL-10 levels and upgrades formation of 15-HETE and LXA4. 2-ARA-LysoPtdEtn can be used for the research of peritonitis.
  • HY-180363
    E 6080 Inhibitor
    E 6080 is an orally active and selective 5-lipoxygenase (5-LOX) inhibitor with an IC50 of 0.2 μM in rat basophilic leukemia cell. E 6080 shows potent inhibitory effects on the release of leukotrienes. E 6080 inhibits the bronchospasm induced by antigen (ovalbumin) inhalation in sensitized conscious guinea pigs. E 6080 can be used for the study of asthma.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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-16344
    Nedocromil sodium Inhibitor
    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • 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.
  • 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-119442
    Quininib Antagonist 98.1%
    Quininib is a cysteinyl leukotriene 1 and 2 receptor antagonist with IC50s of 1.2 and 52 μM for CysLT1R and CysLT2R, respectively. Quininib is a potent inhibitor of developmental angiogenesis in the zebrafish eye. Quininib can be used for the research of ocular neovascular pathologies and may complement current anti-VEGF biological agents.
  • HY-123816
    ONO 2050297 Inhibitor
    ONO 2050297 (Compound 19) is a selective Cysteinyl leukotriene (CysLT) antagonist with IC50s of 17  and 0.87 nM for CysLT1 and CysLT2, respectively. ONO 2050297 can be used for bronchial asthma research.
  • HY-176921
    ONO-2570366 Antagonist
    ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC50 = 14 nM). ONO-2570366 inhibits the binding of LTD4
  • HY-101731
    CP-96021 hydrochloride Antagonist
    CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Ki values of 34 nM and 37 nM, respectively.