LTB₄ Antagonist

CP-105696 is a potent and selective Leukotriene B₄ Receptor antagonist, with an IC₅₀ of 8.42 nM.

LY255283 is a LTB₄ receptor (BLT2) antagonist, with an IC₅₀ of ~100 nM for [³H]LTB₄ binding to guinea pig lung membranes.

Etalocib (LY293111), an orally active leukotriene B₄ receptor antagonist, inhibits the binding of [³H]LTB₄, with a K_i of 25 nM. Etalocib (LY293111) prevents LTB₄-induced calcium mobilization with an lC₅₀ of 20 nM. Etalocib (LY293111) induces apoptosis.

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 K_i values of 1.7 nM.

Amelubant (BIIL 284) is a potent, oral and long acting LTB₄ receptor antagonist, negligibly binds to LTB₄ receptor, with K_is of 221 nM and 230 nM in vital cells and membranes. Amelubant (BIIL 284) is a proagent of active metabolites BIIL 260 and BIIL 315. Anti-inflammatory activity.

SB-209247 is a selective, high affinity and orally active leukotriene B4 (LTB4) receptor antagonist with a K_i of 0.78 nM. SB-209247 blocks LTB4-induced Ca²⁺ mobilization with an IC₅₀ of 6.6 nM. SB-209247 shows a potent anti-inflammatory activity.

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.

ONO4057 is a Leukotriene B₄ receptor antagonist, with an IC₅₀ of 0.7±0.3 μM.

SB-201993 is a selective leukotriene B₄ (LTB4) receptor antagonist with a K_i=7.6 nM for LTB4 receptors on human inflammatory cells. SB-201993 inhibits calcium mobilization in inflammatory cells and 5-lipoxygenase activity, exerting anti-inflammatory effects. SB-201993 is promising for research of inflammatory diseases (e.g., dermatitis, arthritis).

Etalocib (LY293111) sodium, an orally active leukotriene B₄ receptor antagonist, inhibits the binding of [³H]LTB₄, with a K_i of 25 nM. Etalocib sodium prevents LTB₄-induced calcium mobilization with an lC₅₀ of 20 nM. Etalocib sodium induces apoptosis.

LTB4 antagonist 1, a carboxamide-acid compound, is a potent Leukotriene B4 (LTB4) antagonist with an IC₅₀ of 288 nM. LTB4 antagonist 1 has significant anti-inflammatory properties.

DW-1350 is a LTB₄ receptor antagonist.

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 K_i 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.

14,15-Dehydro Leukotriene B4 (Compound 4) is a LTB4 receptor antagonist. 14,15-Dehydro Leukotriene B4 also has a higher binding affinity for BLT1 with a K_i value of 27 nM and BLT2 with a K_i value of 473 nM. 14,15-Dehydro Leukotriene B4 inhibits LTB4-induced release of lysozymes from rat polymorphonuclear leukoctyes with an IC₅₀ value of 1 µM.

LTB4 antagonist 2, a carboxamide-acid compound, is an antagonist of leukotriene B4 (LTB4) with potentially anti-inflammatory activity. LTB4 antagonist 2 shows good affinity for the LTB4 receptor with IC₅₀ of 439 nM.

SM-15178 is a potent, orally active and selective leukotriene B₄ (LTB₄) receptor antagonist with an IC₅₀ of 0.30 μM. SM-15178 attenuates LTB₄ (HY-107608)-induced neutrophil accumulation in mouse skin and bronchoconstriction in guinea pigs. SM-15178 emonstrates significant anti-inflammatory efficacy across multiple animal models of inflammation. SM-15178 can be used for the research of chronic inflammatory diseases such as inflammatory bowel disease, psoriasis, and asthma.

LY210073 is a Leukotriene B₄ (LTB₄) receptor antagonist with an IC₅₀ of 6.2 nM.