LTC₄/CysLT₂ Antagonist

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.

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 K_is of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.

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.

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 K_is of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.

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.

(Rac)-HAMI 3379 is the racemate of HAMI 3379. HAMI 3379 is a potent and selective Cysteinyl leukotriene (CysLT₂) receptor 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.

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.

CysLT1/2 receptor antagonist-1 is a dual CysLT1 and CysLT2 receptor antagonist with IC₅₀ values of 0.044 μM (CysLT1) and 0.17 μM (CysLT2). CysLT1/2 receptor antagonist-1 can be used for the research of bronchial asthma.

ONO-2570366 (Compound 11a) is an antagonist of the cysteinyl leukotriene receptors CysLT1R and CysLT2R (IC₅₀ = 14 nM). ONO-2570366 inhibits the binding of LTD₄asthma.

CP-96021 hydrochloride is a balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with K_i values of 34 nM and 37 nM, respectively.

BRI-12349 (Compound 50) is a dual antagonist of CysLT1R/CysLT2R with K_i values of 1.03 and 6.46 μM. BRI-12349 can inhibit the generation of IP₁ induced by LTD₄ (the main ligand of CysLTs). BRI-12349 can be used for the research of immunology and inflammation, such as asthma.

LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for ³H-LTC4 sites.