Catalog No.
Product Name
Application
Product Information
Citations
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mast cell stabilizer
Nedocromil is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade. -
LTD4 receptor antagonist
Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist. -
CysLT1 receptor antagonist
Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist. -
LTD4 receptor antagonist
Verlukast (MK-0679) is a potent leukotriene D4 antagonist -
PGF2α/LTB4 production inhibitor
Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM). -
Leukotriene receptor antagonist
Pranlukast is a selective cysteinyl leukotriene receptor antagonist. -
CysLT1 receptor antagonist
MK-571 is a potent CysLT1 (LTD4) leukotriene receptor inverse agonist with EC50 value of 1.3 nM.- Jung-Hung Chen, .et al. , Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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CysLT1 receptor antagonist
MK-571 is a selective, orally active CysLT1 receptor antagonist. It blocks the binding of LTD4, but not LTC4, to human and guinea pig lung membranes with Ki values of 0.22 nM and 2.1 nM, respectively. -
LTR antagonist
Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. -
5-Lipoxygenase (5-LO) inhibitor
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation. -
peptidoleukotrienes antagonist
RG-12525 is a a specific, competitive and orally effective antagonist of the peptidoleukotrienes, LTC4, LTD4 and LTE4, inhibiting LTC4-, LTD4- and LTE4-inducd guinea pig parenchymal strips contractions, with IC50s of 2.6 nM, 2.5 nM and 7 nM, respectively; RG-12525 is also a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist with IC50 of appr 60 nM and a potent inhibitor of CYP3A4, with a Ki value of 0.5 ?M. -
leukotriene A4 hydrolase inhibitor
Acebilustat (CTX-4430) is a leukotriene A4 hydrolase inhibitor, used for an oral antiinflammatory drug. -
CysLT1/CysLT2 antagonist
Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively. -
leukotriene receptor antagonist
Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma. -
LTB4 antagonist
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. -
LTC4 inhibitor
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2). -
leukotriene B4 receptor antagonist
Etalocib, also known as LY293111 and VML295, is a potent and selective inhibitor of the lipoxygenase pathway either directly through 5'-lipoxygenase or via antagonism of the leukotriene B4 (LTB4) receptor. -
Protein Kinase C Inhibitor/LTD4 Antagonist
LY 170198 is a potent protein kinase C inhibitor and LTD4 antagonist. This compound exhibits significant biological activity relevant to studies on tumor promotion, oncogene activation, and protein phosphorylation. Additionally, it is valuable for investigating feedback mechanisms in signal transduction pathways and cellular responses to growth factors, making it a useful tool for cancer research and related fields. -
LTB4 inhibitor
U-75302 is a potent inhibitor of leukotriene B4, developed as a pyridine analogue. This compound demonstrates significant anti-inflammatory activity, making it valuable for research into various inflammatory diseases. U-75302 can help elucidate the role of leukotriene B4 in pathophysiological processes, contributing to better understanding and potential therapeutic strategies in inflammation-related conditions. -
LTB4 Antagonist
γ-Linolenic acid ethyl ester serves as a leukotriene B4 receptor 4 (LTB4) antagonist. This compound exhibits anti-inflammatory properties by inhibiting LTB4 signaling pathways, which are implicated in various inflammatory conditions. Its applications in research include studying immune responses and exploring therapeutic avenues for inflammation-related diseases. -
BLT1 Antagonist
Moxilubant is a potent BLT1 antagonist, exhibiting a competitive inhibition of LTB4 signaling with an efficacy of 2-4 nM. This compound effectively inhibits LTB4-induced neutrophil activation and functions, making it a valuable tool in the study of inflammatory responses. Research applications include investigations into chronic obstructive pulmonary disease and related conditions characterized by neutrophil-mediated inflammation. -
LTB4 Metabolite
20-Carboxy-Leukotriene B4 is a key metabolite of Leukotriene B4 that targets the BLT1 receptor, demonstrating high affinity binding. This compound effectively inhibits LTB4-mediated neutrophil responses, including migration, degranulation, and leukotriene biosynthesis. It is valuable in research applications focused on inflammation, immune response modulation, and the study of leukotriene signaling pathways. -
Leukotriene D4/E4 Antagonist
Tomelukast is an orally active antagonist of leukotriene D4 and E4, primarily involved in mediating inflammatory responses in asthma. This compound inhibits the action of leukotrienes, thereby reducing bronchoconstriction and inflammatory cell recruitment in the airways. Tomelukast is useful in research applications focused on asthma pathophysiology and the evaluation of anti-inflammatory therapies. -
PGF2α/LTB4 Inhibitor
Darbufelone is a dual inhibitor of prostaglandin F2α (PGF2α) and leukotriene B4 (LTB4) production, primarily targeting the cyclooxygenase enzyme PGHS-2 with an IC50 of 0.19 μM, while showing markedly lower potency against PGHS-1 (IC50 of 20 μM). This compound is valuable for research focused on inflammation, pain modulation, and the role of eicosanoids in various pathological conditions. Its selective inhibition of PGF2α and LTB4 makes Darbufelone a useful tool for studying the intersection of these signaling pathways in cellular responses. -
Unsaturated Fattly Acid
11(Z),14(Z)-Eicosadienoic acid is an unsaturated fatty acid that selectively inhibits [3H] leukotriene B4 (LTB4) binding to pig neutrophil membranes, with a binding affinity characterized by a Ki of 3 μM. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research focused on inflammatory processes and leukotriene signaling pathways. Its ability to modulate leukotriene interactions supports its use in studies of immune response and related therapeutic areas. -
LTD4/E4 Receptor Antagonist
Ritolukast is a potent antagonist of the LTD4/E4 leukotriene receptors. This compound demonstrates significant biological activity by inhibiting bronchoconstriction induced by aerosolized LTD4, with an ID50 of 0.5 mg/kg in guinea pigs. Ritolukast is primarily utilized in research applications related to respiratory pharmacology and the study of allergic inflammatory responses. -
FPR Inhibitor
Boc-Phe-Leu-Phe-Leu-Phe (Boc-FLFLF) acts as an inhibitor of N-formyl peptide receptors (FPR). This compound effectively reduces FMLP-induced release of peptide leukotrienes and disrupts the sprouting of human umbilical vein endothelial cell (HUVEC) spheroids in a three-dimensional fibrin gel model, which simulates the conditions associated with proliferative diabetic retinopathy (PDR) and vascular endothelial growth factor (VEGF). Additionally, Boc-Phe-Leu-Phe-Leu-Phe counteracts the anti-inflammatory and antifibrotic effects of Ac2-26. It is suitable for applications in immunological research. -
CysLT Receptor Antagonist
BAY-u 9773 is a non-selective antagonist of the cysteinyl leukotriene (CysLT) receptors, effectively inhibiting both CysLT1 and CysLT2 with comparable IC50 values. This compound is utilized in research to study leukotriene-mediated processes and to explore therapeutic strategies for conditions associated with cysteinyl leukotrienes, such as asthma and allergic responses. -
CysLT2 Receptor Antagonist
BayCysLT2 is a selective and potent antagonist of the cysteinyl leukotriene 2 (CysLT2) receptor, exhibiting an IC50 value of 53 nM. It effectively inhibits calcium mobilization induced by leukotriene D4 in HEK293 cells expressing human CysLT2 receptors. Additionally, BayCysLT2 demonstrates the ability to reverse LTC4-induced increases in coronary artery perfusion pressure and decreases in contractility in isolated guinea pig hearts, making it valuable for research on cardiovascular and inflammatory responses. -
Leukotriene Receptor Antagonist
KP496 is a selective dual antagonist targeting the Leukotriene D4 receptor and Thromboxane A2 receptor. It exhibits significant inhibition of leukotriene-mediated inflammatory responses, making it valuable in studies of allergic reactions and asthma. This compound is essential for research exploring therapeutic strategies for inflammation-related diseases. -
LTB4 Receptor Antagonist
SB-209247 is a selective leukotriene B4 (LTB4) receptor antagonist, exhibiting high affinity with a Ki of 0.78 nM. This compound effectively inhibits LTB4-induced calcium mobilization, with an IC50 of 6.6 nM, displaying significant anti-inflammatory properties. SB-209247 is valuable for research applications focusing on inflammatory diseases and the modulation of leukotriene signaling pathways. -
LTB4 Inhibitor
Halometasone is a corticosteroid that functions as an inhibitor of leukotriene B4 (LTB4) synthesis. It exhibits anti-inflammatory properties by reducing LTB4 and thymic stromal lymphopoietin (TSLP) levels. Halometasone is widely utilized in research related to psoriasis and other eczematous skin disorders, providing insights into corticosteroid-mediated effects on inflammatory pathways. -
BLT2 Agonist
CAY10583 is a potent and selective full agonist of the Leukotriene B4 receptor type 2 (BLT2). This compound effectively promotes keratinocyte migration in vitro and enhances wound healing in vivo, making it a valuable tool for studies on tissue repair mechanisms. CAY10583 holds potential for therapeutic applications in the treatment of diabetic wounds and related conditions. -
HAMI 3379 Racemate
(Rac)-HAMI 3379 is a racemic mixture of HAMI 3379, a potent and selective antagonist of the Cysteinyl leukotriene 2 (CysLT2) receptor. This compound exhibits significant biological activity in modulating inflammatory processes linked to allergic responses and asthma. It is valuable for research applications focused on understanding the role of leukotrienes in various pathological conditions. -
LTD4/LTE4 Antagonist
SR2640 hydrochloride is a potent and selective competitive antagonist of leukotriene D4 and leukotriene E4. This compound is invaluable for studying the role of leukotrienes in asthma and may provide insights into inflammatory pathways associated with respiratory diseases. Its well-defined mechanism makes it a useful tool for pharmacological research and the development of therapeutic strategies targeting leukotriene-mediated responses.
