Leukotriene Receptor

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.

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

Etalocib (LY293111) is a novel diaryl ether carboxylic acid derivative, is a selective and potent inhibitor of the lipoxygenase pathway either via antagonism of the leukotriene B4 (LTB4) receptor or directly through 5'-lipoxygenase. It has antineoplastic activities.

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

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.

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

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.

CGP 35949 is an LTD4 antagonist with phospholipase inhibitory activity.

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.

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.

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.

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.

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

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.

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

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

L 674573 is an inhibitor of leukotriene biosynthesis.

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.

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

REV 5901A (REV 5901 HCl) is an orally active leukotriene receptor antagonist and 5-lipoxygenase inhibitor with antimicrobial activity that attenuates colon cancer growth in mice.REV 5901A has been used in studies of asthma and myocardial infarction. REV 5901A is used to study asthma and myocardial infarction.

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

AZD9898 is an inhibitor of leukotriene-C4 synthetase with an IC50 of 0.28 nM. AZD9898 can be used in studies about asthma. AZD9898 mitigates the GABA binding and hepatic toxicity signal.

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.

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.

RS-601 is a potent dual leukotriene D4 thromboxane A2 inhibitor that inhibits antigen-induced airway hyperresponsiveness (AHR) and shows asthmatic effects in a guinea pig model of asthma.

Tipelukast (KCA 757) is a novel, orally available leukotriene receptor antagonist with anti-inflammatory properties, capable of reducing fibrosis and down-regulating TIMP-1 and type 1 collagen. Tipelukast is utilized in asthma research.

Compound 24e, a leukotriene B4 (LTB4) antagonist, exhibits an inhibitory concentration 50 (IC50) of 477 nM and demonstrates anti-inflammatory activity [1].

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM without affecting CHO-BLT1 cell chemotaxis. It blocks the interaction between LTB4 and the BLT2 receptor with a K_i of 132 nM and may serve as a research tool for inflammatory airway diseases, including asthma and chronic obstructive pulmonary disease [1].

BLT2 Probe 1 (Compound 13), a fluorescent probe derived from the synthetic BLT2 agonist CAY10583, offers a robust tool for exploring BLT2 receptor ligand pharmacology across various assay systems [1]. As BLT2 is a valuable target for treatments in diabetic wound healing and gastrointestinal lesions, this probe facilitates relevant biomedical research.

LTB4 antagonist 2, a carboxamide-acid compound, serves as an antagonist to leukotriene B4 (LTB4) with potential anti-inflammatory properties, exhibiting high affinity for the LTB4 receptor and an inhibitory concentration (IC50) of 439 nM [1].

LTB4 Antagonist 1, a carboxamide-acid derivative, potently inhibits Leukotriene B4 (LTB4) activity with an IC50 value of 288 nM and exhibits notable anti-inflammatory properties [1].