leukotriene b4

Leukotriene B4 (LTB4) is a compound derived from arachidonic acid via the 5-lipoxygenase pathway that mediates certain inflammatory and immune responses. Leukotriene B4 induces neutrophil extracellular traps that impede the clearance of Pneumocystis japonicus.

6-trans-Leukotriene B4 is a neutrophil chemotactic agent present in guinea pig dermis.

12-oxo Leukotriene B4 (12-Oxo-LTB4) is a potent pro-inflammatory lipid mediator classified as a dihydroxy fatty acid that is enzymatically derived from arachidonic acid metabolism via the 5-lipoxygenase (5-LO) pathway, and it promotes a diverse array of leukocyte functional responses including cellular aggregation, stimulation of transmembrane ion fluxes, enhancement of lysosomal enzyme release, superoxide anion generation, chemotaxis, and chemokinesis; 12-oxo Leukotriene B4 is an initial oxidative metabolite formed from Leukotriene B4 via the LTB4 12-hydroxydehydrogenase pathway, which undergoes rapid enzymatic conversion first to 10,11-dihydro-12-oxo-LTB4 followed by reduction of the 12-oxo group to yield 10,11-dihydro-LTB4, and this metabolite exhibits significantly reduced biological potency, being approximately 70-fold less potent than LTB4 in stimulating Ca2+ mobilization in human neutrophils (EC50 = 33 nM vs. 0.46 nM) and also markedly less effective at stimulating neutrophil migration (EC50 = 170 nM vs. 2.7 nM).

Leukotriene B4 (LTB4) is a dihydroxy fatty acid derived from arachidonic acid through the 5-lipoxygenase pathway. It promotes a number of leukocyte functions including aggregation, stimulation of ion fluxes, enhancement of lysosomal enzyme release, superoxide anion production, chemotaxis, and chemokinesis. At least two LTB4 receptors, termed BLT1 and BLT2, have been identified. 14,15-dehydro LTB4 is a LTB4 receptor antagonist that has a higher binding affinity for BLT1, demonstrating a Ki value of 27 nM, compared to BLT2, which has a Ki value of 473 nM. 14,15-dehydro LTB4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC50 value of 1 μM.

LTB4 dimethyl amide is a moderate inhibitor of LTB4-induced degranulation of human neutrophils (Ki = 130 nM) and lysozyme release from rat PMNL. LTB4 dimethyl amide appears to be an antagonist of the LTB4 receptor on guinea pig lung membranes.

The effects of Leukotriene B4 (LTB4) are mediated by two known receptors, BLT1 and BLT2. LTB4 is a high affinity ligand for BLT1, and many of its pro-inflammatory effects are believed to be transduced through this receptor. The BLT2 is more enigmatic, in that LTB4 is not a high-affinity ligand, nor is it clear that BLT2 activation promotes inflammation. LTB4 ethanolamide (LTB4-EA) is a theoretical 5-LO metabolite of arachidonoyl ethanolamide (AEA). In CHO cells transfected with human BLTR1, LTB4-EA was a potent antagonist with about three times greater affinity for the receptor than LTB4 (Ki = 1.22 nM versus 3.88 nM). LTB4-EA antagonizes the LTB4-induced contractions of guinea pig lung parenchyma with an EC50 of 10 nM. LTB4-EA thus represents a potential endogenous anti-inflammatory compound functioning as a natural antagonist of BLTR1.

Leukotriene B4 (LTB4) compounds are produced by both enzymatic and non-enzymatic processes. The products of enzymatic origin, via Leukotriene A4 (LTA4) hydrolase, are stereospecifically 12(R). Non-enzymatic hydrolysis products are 50:50 mixtures at C-12, but are almost exclusively trans at C-6. Thus, the non-enzymatic hydrolysis product of LTA4 is 6-trans-12-epi LTB4. 12-epi LTB4 is an isomer which would not be expected to occur in either non-enzymatic hydrolysis products, or in the enzymatic products of LTA4 hydrolase. Compared to LTB4, 12-epi LTB4 has significantly reduced activity for the LTB4 receptor on human neutrophils (IC50 of 7.5 mM), and on guinea pig lung membranes with a (Ki of 4.7 mM). 12-epi LTB4 is an weak agonist at both the recombinant human BLT1 and BLT2 receptors, requiring approximately 10 mM for full activation of the receptor.

20-hydroxy LTB4 is a metabolite of LTB4 in human neutrophils. In human leukocytes, LTB4 is inactivated by the enzyme LTB4 20-hydroxylase. 20-hydroxy LTB4 is not only much less active (~5%) compared to LTB4 in causing degranulation of PMNL, but actually inhibits LTB4-induced degranulation of human neutrophils (Ki = 13.3 nM). However, 20-hydroxy LTB4 is as active as LTB4 in contracting parenchymal strips from guinea pig lung. 20-hydroxy LTB4 retains considerable ligand binding affinity at the BLT2 receptor, but does not appear to function as an agonist.

6-trans-12-epi-Leukotriene B4, a metabolite of arachidonic acid, acts as a potent anti-inflammatory agent.

20-Carboxy-Leukotriene B4 (20-COOH LTB4), a metabolite of Leukotriene B4 (LTB4), exhibits high affinity for the BLT1 receptor and significantly inhibits LTB4-mediated neutrophil responses such as migration, degranulation, and leukotriene biosynthesis [1].

Leukotriene B4 (LTB4)-3-aminopropylamide is an analog of LTB4 that exhibits potent and selective binding to the BLT1 receptor with Ki values of 5.1 nM at BLT1 and 1,227 nM at BLT2, indicating its high affinity for BLT1 over BLT2. This compound's effects are mediated through interactions with two receptors, BLT1 and BLT2.

18-Carboxy dinor Leukotriene B4 (18-carboxy dinor LTB4) represents a β-oxidation metabolite of Leukotriene B4 (LTB4). Initially, LTB4 is metabolized in the liver to 20-carboxy LTB4, which subsequently undergoes β-oxidation to form 18-carboxy dinor LTB4.

20-trifluoro Leukotriene B4 is an active molecule that can be used in life science related research. The CAS number of 20-trifluoro Leukotriene B4 is 115178-97-7.

5-Oxo Leukotriene B4 (5-oxo LTB4) serves as an intermediate metabolite in the production of 12-oxo LTB4.

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.

Bunaprolast (U66858) is a novel and potent leukotriene B4 (LTB4) inhibitor.Bunaprolast exhibits oxidative degradation activity and inhibits lipoxygenase and TXB2 release.

CJ-13,610 is an orally active and nonredox-type inhibitor of 5-lipoxygenase (5-LOX). CJ-13,610 inhibits the biosynthesis of leukotriene B4 and regulates the expression of IL-6 mRNA in macrophages.

Ticolubant is orally active leukotriene B4 antagonist with high affinity for the human neutrophil LTB4 receptor (Ki = 0.78 nM), blocks LTB4-induced Ca2+ migration with an IC50 of 6.6 ± 1.5 nM, and shows topical anti-inflammatory activity in a mouse model of skin inflammation.

Moxilubant is a small molecule leukotriene B4 receptor 1 (LTB4R) antagonist for the treatment of immune system disorders, skin and musculoskeletal disorders, and may be used in studies of psoriasis and rheumatoid arthritis.

Ontazolast is a small molecule leukotriene B4 receptor (LTB4R) antagonist for the treatment of immune system disorders and respiratory diseases.Ontazolast is a candidate compound for the treatment of asthma.

BIRM 271 is a novel arachidonic acid release inhibitor that blocks leukotriene B4 and platelet-activating factor biosynthesis in human neutrophils. BIRM 271 and BIRM 270 are enantiomers that inhibit the production of leukotriene B4 with IC50 of 40 nM.

Croconazole exhibited dose-dependent inhibitory activity on the 5-lipoxygenase (5-LOX) of neutrophils. Croconazole is an antimycotic agent. The IC50s for the synthesis of leukotriene B4 (LTB4) and 5-hydroxyeicosatetraenoic acid (5-HETE) is 7.8 +/- 1.7 and

Sulfasalazine (Azulfidine) is a synthetic salicylic acid derivative with affinity for elastin-containing connective tissues and formulated as a prodrug. Sulfasalazine induces iron death and inhibits NF-κB, TGF-β and COX-2.

BIIL-260 hydrochloride is an orally active and highly efficient leukotriene B4 (LTB4) receptor antagonist with anti-inflammatory activity. It interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, inhibiting LTB4-induced intracellular Ca2+ release in human neutrophils.