leukotriene a4

SC 57461A is a potent and specific leukotriene A4 hydrolase (LTA4H) inhibitor.

Leukotriene A4 methyl ester can be converted into leukotriene C4 monomethyl ester catalyzed by the major alkaline cytosolic glutathione transferase in rat liver, which can be used in metabolism-related studies.

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.

DG051 is a potent leukotriene A4 hydrolase (LTA4H) inhibitor with an IC50 of 47 nM.

LYS006 hydrochloride is a potent inhibitor of leukotriene A4 hydrolase (LTA4H) with an IC50 value of 2 nM. It is applicable in the study of inflammatory and autoimmune diseases. For further details, please refer to compound 29 in patent document WO2015092740A1.

4-MDM (4-Methoxydiphenylmethane) is an orally active anti-inflammatory compound that selectively enhances the aminopeptidase activity of leukotriene A4 hydrolase (LTA4H). By promoting the degradation of proline-glycine-proline by LTA4H, 4-MDM reduces neutrophil recruitment in the lungs, alleviating inflammation without affecting the epoxide hydrolase activity of LTA4H. This compound is useful for research in pulmonary diseases.

SC-22716 is an orally active leukotriene A4 (LTA4) hydrolase inhibitor.SC-22716 has potential anti-inflammatory activity and may be used in the study of inflammatory bowel disease and psoriasis.

Lipoxin A4 methyl ester (LXA4 methyl ester) is a more lipid soluble, prodrug formulation of the transcellular metabolite LXA4. LXA4 is a trihydroxy fatty acid containing a conjugated tetraene, produced by the metabolism of 15-HETE or 15-HpETE with human leukocytes.[1] LXA4 is equipotent to leukotriene B4 (LTB4) in inducing superoxide generation in human neutrophils at 0.1 μM.[2] LXA4 is associated with several other biological functions including leukocyte activation, chemotaxis effects, natural killer cell inhibition, and monocyte migration and adhesion.[2],[3],[4]

Acebilustat (CTX-4430) (ZK322) is an effective and specific leukotriene B4 hydrolase inhibitor.

5(S),6(R)-DiHETE is a dihydroxy polyunsaturated fatty acid and a nonenzymatic hydrolysis product of leukotriene A4 (LTA4). Mouse liver cytosolic epoxide hydrolase catalyzes the conversion of LTA4 to 5(S),6(R)-DiHETE. It is a weak LTD4 receptor agonist in guinea pig lung membranes. It induces guinea pig ileum contraction with an ED50 value of 1.3 μM.

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.

5(S)-Hydroperoxyeicosatetraenoic acid (5(S)-HpETE) is a monohydroperoxy polyunsaturated fatty acid (PUFA) generated by the enzymatic conversion of arachidonic acid via 5-lipoxygenase (5-LO). Subsequently, 5(S)-HpETE undergoes metabolism to form leukotriene A4 (LTA4), which serves as a pivotal intermediate in the synthesis of leukotrienes (LTs).

Bestatin trifluoroacetate (Ubenimex trifluoroacetate) is a CD13 (Aminopeptidase N) APN and leukotriene A4 hydrolase inhibitor that is often used in cancer research.

Tosedostat (CHR-2797) is an orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Intracellularly converted into the poorly membrane-permeable active metabolite (CHR-79888), it inhibits puromycin-sensitive aminopeptidase (PuSA) and leukotriene A4 (LTA4) hydrolase. This inhibition in tumor cells may lead to amino acid deprivation, suppressed protein synthesis, increased proapoptotic protein Noxa levels, and ultimately, cell death.

DG-051 is a novel leukotriene A4 (LTA4H) hydrolase inhibitor of leukotriene B4 biosynthesis.

JNJ-26993135 is a potent and selective leukotriene A4 hydrolase (LTA4H) inhibitor.

LTA4H-IN-2 (compound (S)-2) acts as an orally active inhibitor targeting Leukotriene A4 Hydrolase, exhibiting potent activity with an IC 50 of less than 3 nM [1].

LYS006 is a highly efficient and selective LTA4H (leukotriene A4 hydrolase) inhibitor, which can be used for neutrophil-driven inflammatory diseases such as ulcerative colitis.

LYS006 hydrochloride (1799681-85-8 Free base) is a potent LTA4H inhibitor of leukotriene A4 hydrolase. It can be used to study inflammatory and autoimmune diseases, including ulcerative colitis and NASH.