LTD₄/CysLT₁ Antagonist

MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D₄ (LTD₄) receptor antagonist, with K_i 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.

Montelukast (MK0476 free base) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT₁). Montelukast can be used for the reseach of asthma and liver injury. Montelukast also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast decreases eosinophil infiltration into the asthmatic airways. Montelukast can also be used for COVID-19 research.

Zafirlukast (ICI 204219) is a potent orally active leukotriene D₄ (LTD₄) receptor antagonist. Zafirlukast shows anti-asthmatic, anti-inflammatory and anti-bacterial effects.

MK-571 (L-660711) sodium is an orally active, potent and selective competitive leukotriene D₄ (LTD₄) receptor antagonist, with K_i 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.

Montelukast sodium (MK0476) is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT₁). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast sodium decreases eosinophil infiltration into the asthmatic airways. Montelukast sodium can also be used for COVID-19 research.

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.

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.

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.

Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.

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.

CP-96021 is an orally active dual leukotriene D4 (LTD4) and platelet activating factor (PAF) receptor antagonist, featuring a guinea pig LTD4 receptor K_i of 34 nM and a rabbit PAF receptor K_i of 37 nM. CP-96021 blocks ligand binding to its target receptors, inhibits ligand-induced bronchoconstriction, and inhibits antigen-triggered airway obstructive effects. CP-96021 can be used for the research of asthma.

KP496 is a selective, dual antagonist for Leukotriene D4 receptor and Thromboxane A2 receptor.

CAY10789 is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC₅₀=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC₅₀=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases.

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.

Montelukast (MK0476) dicyclohexylamine is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (CysLT₁). Montelukast dicyclohexylamine can be used for the reseach of asthma and liver injury. Montelukast dicyclohexylamine also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage. Montelukast dicyclohexylamine decreases eosinophil infiltration into the asthmatic airways. Montelukast dicyclohexylamine can also be used for COVID-19 research.

CP-288886 is a cysLT₁ receptor antagonist with a K_i value of 0.004 μM. CP-288886 exhibits comparable activity to Zafirlukast (HY-17492) and Pranlukast (HY-B0290). CP-288886 inhibits calcium mobilization with an IC₅₀ of 0.0005 μM in human U937 cells. CP-288886 has high oral bioavailability. CP-288886 possesses anti-asthmatic activity in a guinea pig asthma model and can be used for the research of diseases such as asthma.

L-695499 is a potent and orally active leukotriene D4 receptor antagonist. L-695499 can be used for the researches of inflammation and immunology.

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.

MEN-91507 is an orally activecysteinyl leukotriene receptor 1 (CysLTR1) receptor antagonist. MEN-91507 behaves as insurmountable antagonist of Leukotriene D4 (HY-113456)-induced calcium transients, with a pK_b of 10.25. MEN-91507 can inhibit Leukotriene D4-induced bronchoconstriction and microvascular leakage in guinea-pigs. MEN-91507 can be used for the researches of inflammation, immunology.