Leukotriene Receptor 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.

Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (K_i=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.

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.

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.

CP-105696 is a potent and selective Leukotriene B₄ Receptor antagonist, with an IC₅₀ of 8.42 nM.

LY255283 is a LTB₄ receptor (BLT2) antagonist, with an IC₅₀ of ~100 nM for [³H]LTB₄ binding to guinea pig lung membranes.

Etalocib (LY293111), an orally active leukotriene B₄ receptor antagonist, inhibits the binding of [³H]LTB₄, with a K_i of 25 nM. Etalocib (LY293111) prevents LTB₄-induced calcium mobilization with an lC₅₀ of 20 nM. Etalocib (LY293111) induces apoptosis.

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.

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 K_i values of 1.7 nM.

Resolvin E2 ((-)-Resolvin E2) is an endogenous lipid mediator produced from eicosapentaenoic acid (EPA) under the catalysis of 5-lipoxygenase (5-LOX), and its production increases in hypoxic environments. Resolvin E2 antagonizes BLT1, partially activates ChemR23, and promotes ubiquitin-proteasome-mediated degradation of COX-2. Resolvin E2 reduces the production of prostaglandin E₂, blocks polymorphonuclear leukocyte infiltration, and promotes the resolution of airway inflammation. Resolvin E2 ameliorates lipopolysaccharide (LPS) (HY-D1056)-induced depressive-like behaviors. Resolvin E2 can be used in research related to depression, murine peritonitis, neonatal asthma, and other conditions.

γ-Linolenic acid ethyl ester (Ethyl γ-linolenate) is a leukotriene B₄ receptor 4 (LTB₄) antagonist.

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.

Amelubant (BIIL 284) is a potent, oral and long acting LTB₄ receptor antagonist, negligibly binds to LTB₄ receptor, with K_is 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.

BayCysLT2, an isophthalic acid derivative, is a selective and potent cysteinyl leukotriene 2 (CysLT2) receptor antagonist with an IC₅₀ value of 53 nM. BayCysLT2 inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. BayCysLT2 reverses LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated perfused guinea pig hearts.

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

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