Leukotriene Receptor

ONO4057 is a potent and orally active Leukotriene B4 receptor antagonist with an IC50 value of 0.7±0.3 μM. Immunosuppressive effect of ONO4057 on rat allografts.

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Montelukast (Singular) is an orally available leukotriene receptor antagonist which is widely used for the prophylaxis and chronic treatment of asthma and has been linked to rare cases of clinically apparent liver injury.

Pobilukast (SKF 104353) is a selective cysteinyl leukotriene receptor antagonist that blocks phosphatidylinositol metabolism and leukotriene D-induced thromboxane synthesis, and can be used to study limiting myocardial damage in excessively myocardial reperfusion-injured (MI R) rats.128-63-53-4

Masilukast(MCC-847) is an oral leukotriene D4 (LTD4) receptor antagonist for the study of diseases associated with inflammation.

Zafirlukast (ICI 204219) is an orally active leukotriene D4 receptor (LTD4) antagonist (IC50=0.6 μM). Zafirlukast has anti-asthmatic, anti-inflammatory, and antimicrobial properties and is used in the prevention and treatment of asthma.

L 651896 is a novel leukotriene biosynthesis and 5-lipoxygenase inhibitor for the study of respiratory and cardiovascular diseases.

CGP 35949 is an LTD4 antagonist with phospholipase inhibitory activity.

Parogrelil Free Base (NM-702 Free Base) is a selective phosphodiesterase 3 inhibitor with bronchodilatory and anti-inflammatory effects, inhibits leukotriene (LT)D(4) and histamine-induced constriction of isolated guinea pig tracheal strips, and can be used in the study of bronchial asthma.

Pranlukast (ONO-1078) is a cysteinyl leukotriene receptor-1 antagonist. It antagonizes or reduces bronchospasm caused, principally in asthmatics, by an allergic reaction to accidentally or inadvertently encountered allergens.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

RG-12525(NID 525) is an orally available, selective and competitive leukotriene D (LTD) antagonist that inhibits LTC4, LTD4 and LTE4-induced contraction of guinea pig thin-walled bands, with IC50 values of 2.6 nM, 2.5 nM, and 7 nM, respectively.RG-12525 inhibits CYP3A4, with a Ki value of 0.5 µM. RG-12525 is a novel and potent PPAR-γ agonist (IC50 value of about 60 nM) with species specificity for the study of asthma.

11-Keto-beta-boswellic acid, a novel Nrf2 activator, and a selective 5-lipoxygenase (5-LOX) inhibitor; it exerts dose dependent cardioprotective effect manifested by dose-dependent reduction in serum lactate dehydrogenase

Montelukast sodium (MK0476) is an orally available leukotriene receptor antagonist which is widely used for the prophylaxis and chronic treatment of asthma and has been linked to rare cases of clinically apparent liver injury.

Ablukast (Ro 23-3544) is a leukotriene receptor antagonist that functions as an anti-asthmatic.

AS-35 is an orally effective, potent, and selective antagonist of leukotrienes, antagonizing LTC4-, LTD4-, and LTE4-induced ileum contractions with IC50 values of 8 nM, 4 nM, and 3 nM, respectively. It exhibits antiallergic activities.

5-O-Demethylnobiletin (5-DEMETHYLNOBILETIN) is a natual product, has anti-inflammatory activity, it may act through a direct inhibition of 5-LOX, without affecting the expression of COX-2.

L 674573 is an inhibitor of leukotriene biosynthesis.

RG 7152 is a leukotriene D4 antagonist with anti-asthmatic properties and can be used in the study of asthma.

Nedocromil (FPL 59002) inhibits the action or formation of multiple mediators. Which including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).

LY255283 is a specific antagonit of leukotriene B4 (LTB4) receptor. It inhibits the production of LTB(4) in human peripheral blood polymorphonuclear leukocytes (PMNL) and in monocytes activated by calcium ionophore A23187.

SR 2640 hydrochloride is a competitive antagonist of leukotriene D4 and E4 and can be used in studies about leukotrienes in human asthma.

ABT-080 (VML 530), a leukotriene synthesis inhibitor, is used potentially for treatment of asthma.

Pranlukast hemihydrate (ONO-1078 hemihydrate) is a selective and potent leukotriene (LT) antagonist with anti-asthmatic activity that inhibits [3H]LTD4 and [3H]LTE4 binding to lung membranes and antagonizes LTC4-induced constriction of guinea-pig airways.Pranlukast hemihydrate is used in the study of asthma. Pranlukast hemihydrate is used in the study of asthma.