Leukotriene Receptor Agonist

N-Methyl Leukotriene C4 (N-Methyl-LTC4) is a non-metabolizable LTC4 analog and a selective cysteinyl leukotriene receptor 2 (CysLT2) agonist, with an EC₅₀ of 46.1 nM for mouse CysLT2 and an EC₅₀ value of 122.3 nM for human CysLT2. N-Methyl Leukotriene C4 shows low potency against CysLT1. N-Methyl Leukotriene C4 activates human and mouse CysLT2 receptors, triggering calcium signaling, β-arrestin-2 binding to phosphorylated receptors, vascular leakage, hypotension, tachycardia, contraction of guinea pig ileum and trachea, mild bronchoconstriction, as well as hypertension associated with peripheral vasoconstriction. N-Methyl Leukotriene C4 can be used in research on asthma, rhinitis, sinusitis, cerebral inflammation and edema, pulmonary arterial hypertension, and cardiovascular diseases.

12S-HHT (12(S)-HHTrE) is an enzymatic product of prostaglandin H₂ (PGH₂) derived from cyclooxygenase (COX)-mediated arachidonic acid metabolism. 12S-HHT is an endogenous ligand for BLT2 that fully activates BLT2 in vivo. 12S-HHT suppresses UV-induced IL-6 synthesis in keratinocytes, exerting an anti-inflammatory activity.

Leukotriene E4-d₅ (LTE4-d₅) is the d-₅-labeled Leukotriene E4 (HY-113465). Leukotriene E4 is a stable final metabolite of cysteinyl leukotrienes, produced by immune cells such as mast cells and eosinophils. Leukotriene E4 serves as a key biomarker for evaluating asthma severity, Aspirin (HY-14654) sensitivity, and mast cell activation disorders. Leukotriene E4 is a full functional agonist of CysLT₁R, which induces sustained intracellular calcium mobilization and Erk phosphorylation. Leukotriene E4 mediates inflammation in a P2Y₁₂ receptor-dependent manner. Leukotriene E4 can be used in the research of asthma and non-steroidal anti-inflammatory drug-exacerbated respiratory diseases.

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.

(Rac)-SC-45694 is a racemate of SC-45694. SC-45694 has full LTB4 agonist activity for neutrophil chemotaxis and has antagonist activity against LTB4-induced neutrophil degranulation.

SC-41930 is a orally active eukotriene-B4 receptor antagonist. SC-41930 alleviates inflammation in guinea pig acetic acid-induced colonic inflammation model.

T-10430 is a potent and orally active leukotriene B4 receptor 2 (BLT2) agonist. T-10430 has the potential for the research of psoriasis.

12-epi-LTB4 is an agonist for BLT1 and BLT2. 12-epi LTB4 exhibits a partial agonistic activity against mBLT1 and mBLT2, and induces phosphorylation of extracellular signal-regulated kinase in primary mouse keratinocytes.

YM-17690 is a LTD₄ and LTE₄ agonist, with a pK_i value of 9.28 for [3H]LTD₄. It induces dose-dependent contractions in guinea pig ileum, lung parenchyma, and trachea, with EC₅₀ values of 16, 3.9, and 22 nM, respectively. YM-17690 can be used in research related to asthma and inflammation.