Montelukast sodium is a potent, selective CysLT1 receptor antagonist.
MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
Leukotriene F4 (LTF4), is a lipid that belongs to the Cysteinyl Leukotriene (CysTL) family[1]. Leukotriene F4 induces bronchoconstriction with an ED50 of 16 μg/kg[2]. The precursor of LTF4 is Leukotriene E4 (LTE4), which isformed from the action of a glutamyl transferase[1].
LY 292728 is a potent leukotriene B4 (LTB4) receptor antagonist. LY 292728 binds to human neutrophils with a Ki of 0.47 nM and binds to guinea pig lung membranes with a Ki of 0.04 nM[1].
Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis[1][2][3].
Darbufelone 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).
Tipelukast (KCA 757) is a sulfidopeptide leukotriene receptor antagonist, an orally bioavailable anti-inflammatory agent and used for the treatment of asthma.
BLT2 antagonist-1 (compound 15b) is a selective BLT2 antagonist that inhibits the chemotaxis of CHO-BLT2 cells with an IC50 of 224 nM. BLT2 antagonist-1 does not inhibits the chemotaxis of CHO-BLT1 cells. BLT2 antagonist-1 also inhibits the binding of LTB4 and BLT2 with a Ki value of 132 nM. BLT2 antagonist-1 can be used for the research of the inflammatory airway diseases such as asthma and chronic obstructive pulmonary disease[1].
CAY10583 is a potent and selective full Leukotriene B4 receptor type 2 (BLT2) agonist. CAY10583 directly promotes keratinocyte migration in vitro and accelerates wound closure in vivo. CAY10583 is a promising pharmaceutical agent for diabetic wounds[1].
CP-96486 is a potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonist with Kis of 20 and 24 nM, respectively.
LY 163443 is a selective antagonist of leukotrienes D4 (LTD4) and E4 (LTE4). LY 163443 can antagonize LTD4-induced contractions of guinea pig ileum, trachea, and lung parenchyma. LY 163443 also inhibits tracheal contractions to LTE4[1][2].
BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM[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 in vital cells and membranes. Amelubant (BIIL 284) is a prodrug of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity[1].
U-75302 is a potent inhibitor of leukotriene B4. U-75302 is a pyridine analogue. U-75302 has the potential for the research of inflammatory diseases[1].
A potent inhibitor of developmental angiogenesis in the zebrafish eye, and a cysteinyl leukotriene 1 and 2 receptor (CysLT1 and 2) antaognist with IC50 of 1.2 and 52 uM, respectively; demonstrates significant anti-angiogenic activity in human endothelial cell, murine aortic ring, and murine oxygen-induced retinopathy models of angiogenesis; does not directly target VEGFRs, and inhibits angiogenesis in a range of cell and tissue systems.
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
MK-571 (L-660711) is an orally active, potent and selective competitive leukotriene D4 (LTD4) receptor antagonist, with Ki values of 0.22 and 2.1 nM in guinea pig and human lung membranes, respectively. MK-571 is also a MRP4 and ABCC1 (MRP1) inhibitor. MK-571 inhibits constitutive and antigen-stimulated S1P (sphingosine-1-phosphate) release[1][2][3].
LM-1484 is an antagonist of CysLT1 receptor and displays a higher affinity for 3H-LTC4 sites.
(S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells[1].
Verlukast is a potent, selective, and orally active antagonist of leukotriene receptor. Verlukast has the potential for the research of asthma[1].
CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist (IC50=2.80 μM) and GPBAR1 (G-protein-coupled bile acid receptor 1) agonist (EC50=3 μM). CAY10789 significantly reduces the adhesion of U937 cells to HAEC, reduces the expression of TNF-α. CAY10789 shows very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used for the research of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases[1].
LY223982 is a potent and specific inhibitor of leukotriene B4 receptor, with an IC50 of 13.2 nM against [3H]LTB4 binding to LTB4 receptor.
Pranlukast-d5 (ONO-1078-d5) is the deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63, 0.99, and 5640 nM, respectively.
LY210073 is a Leukotriene B4 (LTB4) receptor antagonist with an IC50 of 6.2 nM.
Olsalazine is a potent inhibitor of macrophages chemotaxis to LTB4 with an IC50 value of 0.39 mM, also reduces the synthesis of 5-hydroxyeicosatetraenoic acid (5-HETE), 11-HETE, 12-HETE, and 15-HETE in polymorphonuclear leukocyte (PMNL) and mononuclear cells (MNL). Olsalazine can be used for researching ulcerative colitis. Anti-inflammatory activity[1][2].
LTB4 antagonist 3 (compound 24e) is a leukotriene B4 (LTB4) antagonist with an IC50 value of 477 nM. LTB4 antagonist 3 has anti-inflammatory activity[1].
CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration[1].
MK-571-d6 (L-660711-d6) sodium salt is the deuterium labeled MK-571 sodium salt. MK-571 sodium salt is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes[1][2].
Quinotolast sodium in the concentration range of 1-100 μg/mL inhibits histamine, LTC4 and PGD2 release in a concentration-dependent manner.
Pranlukast-d4 is deuterium labeled Pranlukast. Pranlukast is a highly potent, selective and competitive antagonist of peptide leukotrienes. Pranlukast inhibits [3H]LTE4, [3H]LTD4, and [3H]LTC4 bindings to lung membranes with Kis of 0.63±0.11, 0.99±0.19, and 5640±680 nM, respectively.