LTR

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.

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.

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

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.

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

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.

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.

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.

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

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.

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.

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.

LTβR-IN-1 is a potent and selective lymphin β receptor (LTβR) inhibitor. LTβR-IN-1 has a selective inhibitory effect on the nuclear translocation of p52 of TNF12A, and has no obvious effect on the nuclear translocation of p65 mediated by TNF-α receptor, but inhibits the nuclear translocation of p52 stimulated by TWEAK or Anti-LTβR. Translocation with IC50 of 10 μM. LTβR-IN-1 regulates the NF-kB signaling pathway through a ligand-independent manner.

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

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

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.

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.

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.

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

DW-1350 is an antagonist of LTB4 receptor.

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

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

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

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.

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.

Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity[1]. Amelubant (BIIL 284) is a potent, oral and long acting LTB4 receptor antagonist, negligibly binds to LTB4 receptor, with Kis of 221 nM and 230 nM

CP-105696 is a potent and selective leukotriene B4 (LTB4) receptor antagonist for the study of allograft rejection.

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

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

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.

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

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.

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

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.

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.