leukotriene d4

Leukotriene D4 (LTD4) is a potent pro-inflammatory mediator formed from arachidonic acid, a bronchoconstrictor, and induces osteoclast senescence.Leukotriene D4 induces transcriptional activity of potentially oncogenic genes and can be used in the study of asthma.

14,15-Leukotriene D4 (14,15-LTD4) is a member of an alternate class of LTs synthesized by a pathway involving the dual actions of 15- and 12-lipoxygenases (15- and 12-LOs) on arachidonic acid via 15-HpETE and 14,15-LTA4 intermediates. 14,15-LTD4 is classified as an eoxin (EXD4), because it is formed mostly by eosinophils. However, mast cells and nasal polyps can synthesize 14,15-LTD4 as well. Little is known about the physiological actions of 14,15-LTD4. It has weak contractile activity on both guinea pig ileum and pulmonary parenchyma in contrast to the effects of 5-LO-derived LTs. However, in an in vitro permeability assay, 14,15-LTD4 can increase vascular permeability of human endothelial cell monolayers, with similar potency to that of 5-LO-derived LTs, resulting in plasma leakage, a hallmark of inflammation.

11-trans Leukotriene D4 (11-trans LTD4) is a C-11 double bond isomer of LTD4. LTD4 undergoes slow temperature-dependent isomerization to 11-trans LTD4 during storage. 11-trans LTD4 retains about 10-25% of the potency for contraction of guinea pig ileum, trachea, and parenchyma compared to LTD4. It exhibits an ED50 ranging between 12-60 nM for contraction of guinea pig trachea.

Leukotriene D4-D5 (Standard) is a reference standard of Leukotriene D4-D5 intended for quantitative analysis, quality control, and related biochemical research applications. Leukotriene D4-d5 is a deuterated form of Leukotriene D4. Leukotriene D4 is one of the components of the slow-reacting substance of anaphylaxis (SRS-A), produced from LTC4 by the metabolism of γ-glutamyl transpeptidase. It is the first cysteinyl leukotriene metabolite of LTC4. The bronchoconstriction and increased vascular permeability induced by Leukotriene D4 contribute to the pathogenesis of asthma and acute hypersensitivity reactions.

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.

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.

Leukotriene-D4-D5 is a deuterated form of Leukotriene D4. Leukotriene D4 is one of the components of the slow-reacting substance of anaphylaxis (SRS-A), produced from LTC4 by the metabolism of γ-glutamyl transpeptidase. It is the first cysteinyl leukotriene metabolite of LTC4. The bronchoconstriction and increased vascular permeability induced by Leukotriene D4 contribute to the pathogenesis of asthma and acute hypersensitivity reactions.

Amlexanox (AA673) is an anti-aphthous ulcer drug. Amlexanox inhibits the synthesis and release of inflammatory mediators, including leukotrienes and histamine, from mast cells, neutrophils, and mononuclear cells. Amlexanox also acts as a leukotriene D4 antagonist and a phosphodiesterase inhibitor. Amlexanox decreases the time ulcers take to heal as well as the pain associated with the ulcers.

CP-96021 hydrochloride is a potent and orally active antagonist of leukotriene D4 (LTD4)/platelet activating factor receptor (Kis: 34 nM and 37 nM).

CP-96486 is a potent and orally active antagonist of leukotriene D4 (LTD4) and platelet activating factor (PAF) receptors, with inhibitory constants (Kis) of 20 and 24 nM, respectively.

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

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

Pirodomast is a thromboxane A (TXA2) synthase inhibitor. Pirodomast inhibits leukotriene (LT) D4, C4, E4 formation and thromboxane B2 (TXB2) activity, but is weakly or ineffectively antagonistic to guinea pig bronchospasm induced by histamine, methacholine, serotonin, LTC4, or platelet-activating factor. Pirodomast is a potential antiallergic compound. Pirodomast had only weak relaxant activity on guinea pig trachea in vitro. Pirodomast is a potential antiallergic compound that inhibits the protein hydrolyzing activity of trypsin in vitro, prevents antigen-induced immediate and late asthmatic responses in allergic sheep in vivo, and inhibits antigen-induced airway hyperresponsiveness to histamine and carbachol in allergic sheep.

Cilastatin (MK0791) is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibits the metabolism of leukotriene D4 to leukotriene E4.

CI-949 is an allergic mediator release inhibitor that inhibits the release of leukotriene C4/D4 (LTC4/LTD4), histamine, and thromboxane B2 (TXB2) with IC50 values of 0.5 μM, 11.4 μM, and 0.1 μM, respectively.

LTD4 antagonist 1 is a potent and orally active antagonist of leukotriene D4 (LTD4; Ki: 0.57 nM).

KP496 is a selective, dual antagonist for the Thromboxane A2 receptor (TP) and the Leukotriene D4 receptor (cysLT1).

Verlukast (MK-0679) is a selective, orally active leukotriene D4 receptor antagonist for use in bronchial asthma research.

LTD4 antagonist 2 (compound 6) functions as a leukotriene D4 (LTD4) antagonist with an IC50 of 2.8 μM for the cysteinyl leukotriene 1 receptor (CysLT1R). Additionally, it acts as an agonist for the G protein-coupled bile acid receptor 1 (GPBAR1), making it applicable for research into colitis, metabolic syndrome, and other GPBAR1- and CysLT1R-related diseases.

KF-17625 is an orally active bronchodilator. It inhibits bronchoconstriction induced by Carbachol, Histamine, or Leukotriene D4. Additionally, KF-17625 suppresses phosphodiesterase (PDE) IV in canine trachea with an IC50 of 12 μM and reduces histamine release from rat mast cells induced by Concanavalin-A at a 10 μM concentration with a 44% inhibition rate. This compound is applicable in research related to immunology and inflammation.

L-695499 is a potent and orally active antagonist of the leukotriene D4 (LTD4) receptor. It is suitable for use in research related to inflammation and immunology.

LY171883 is an orally active leukotriene D4 and E4 antagonist that can be used in asthma research.

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

L 648051 is a leukotriene D4 receptor antagonist.