LTR

LTB4-IN-1 (Anti-inflammatory agent 2) with IC50 of 70 nM is an inhibitor of leukotriene synthesis (LTB4).

MCI826 is a potent and selective antagonist of P-glycoprotein (P-gp) and peptide leukotrienes (p-LTs), showing anti-asthmatic activity in a guinea pig model of advanced asthma.

CP-105696 is a potent and selective leukotriene B4 (LTB4) receptor antagonist used to study allograft rejection.

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.

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.

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 571 (L660711) is an orally active antagonist of CysLT1 receptor.

YM 16638 is an orally active leukotriene (LT) antagonist with triglyceride-lowering and peroxisome-increasing effects that can be used to study antigen-induced early and late airway responses in allergic sheep.

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.

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

Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.

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

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.

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.

FPL 55712 is a leukotriene receptor and SRS-A antagonist that inhibits bronchoconstriction and can be used in studies of asthma and coronary artery thrombosis.

Darbufelone mesylate (CI-1004 mesylate) inhibited PGF2α and LTB4 in cells and demonstrated IC50 values of 0.19 μM for PGHS-2 and 20 μM for PGHS-1.

HAMI 3379 (HAMI3379) is a selective cysteinyl leukotriene receptor 2 (CysLT2) antagonist that dose- and time-dependently attenuates brain damage and inhibits microglial cell inflammation following focal cerebral ischemia in rats and attenuates ischemia-like neuronal damage by inhibiting microglial activation.

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.

γ-Linolenic Acid methyl ester (Methyl gamma-linolenate) is a weak leukotriene B4 (LTB4) receptor antagonist.

Hnps-PLA Inhibitor is an inhibitor of human nonpancreatic secretory Phospholipase A (hnps-PLA).

Tebufelone is a potent in vitro inhibitor of CO , a novel non-steroidal anti-inflammatory drug (NSAID) belonging to the di-tert-butylphenol (DTBP) class that has shown potent anti-inflammatory, analgesic and anti-reticulitis properties in various animal models. Tebufelone potently inhibits the formation of prostaglandins (PGE2) and blocks the formation of lipoxygenase pathway products [leukotriene (LTB4)] in rat macrophages (IC50 = 20 microM) and human whole blood (IC50 = 22 microM) in vitro. = 20 microM) and human whole blood (IC50 = 22 microM) from the formation of lipoxygenase pathway products [leukotriene (LTB4)] in vitro.

Diffractaic Acid (NSC 685595) can inhibit LTB4 biosynthesis in A-23187-stimulated bovine PMNL cells with activity value of 8 μM.

3-(4-hydroxyphenyl)-1-propanol is a member of the class of compounds known as 1-hydroxy-2-unsubstituted benzenoids.

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.

Linetastine (TMK-688) is a 5-lipoxygenase inhibitor (5-LOX) that inhibits leukotriene production and antagonizes the effects of histamine.Linetastine is used in studies of asthma, atherosclerosis, and peptic ulcers.

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor with a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, without affecting the nuclear translocation of p65 mediated by the TNF-α receptor. It inhibits p52 nuclear translocation stimulated by TWEAK or Anti-LTβR with an IC50 of 10 μM and regulates the NF-kB signaling pathway in a ligand-independent manner.

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.

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

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.

Moxilubant HCl 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.

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.

Ergosta-7,22-dien-3-one is a lanosterane that can be isolated from the substrates of Ganoderma taiwanensis. It exhibits pro-inflammatory properties, stimulating nitric oxide production, inducing gene expression, and promoting the production of TLRs, cytokines, chemokines, and cellular adhesion molecules.

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.

12-OxoETE is an endogenous metabolite formed during the metabolism of arachidonic acid and is present in human platelets and Aplysia nervous tissue .12-KETE induces transient changes and aggregation of intracytoplasmic free calcium ion concentration via leukotriene B4 (LTB4) receptor or coactivation sequences to achieve a rapid and dose-dependent increase.

Veliflapon is an orally active and selective inhibitor of 5-lipoxygenase activating protein (FLAP). Veliflapon inhibits the synthesis of the leukotrienes B4 and C4.

DW-1350 is an antagonist of LTB4 receptor.

Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315 with anti-inflammatory activity[1]. It is a potent, oral, long-acting LTB4 receptor antagonist that negligibly binds to the LTB4 receptor, exhibiting Kis of 221 nM and 230 nM in vital cells and membranes.

LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (Ki: 6.5 nM) with antitumor activity.

Hinokiresinol is a novel inhibitor of LTB4 binding to the human neutrophils, it has antiallergic effect, it inhibits IgE-induced mouse passive cutaneous anaphylaxis reaction. Hinokiresinol (trans-hinokiresinol) and nyasol (cis-hinokiresinol) are estrogen

Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.