E-6123 is a platelet activating factor inhibitor potentially for the treatment of asthma. E6123 inhibited PAF inhalation-induced bronchoconstriction in guinea pigs with an ED50 value (p.o.) of 1.3 micrograms/kg which was lower than those of other PAF-antagonists such as WEB2347 (ED50 = 26 micrograms/kg) and Y-24180 (ED50 = 12 micrograms/kg). E6123 significantly inhibited PAF inhalation-induced eosinophil infiltration into the bronchiole and trachea, and bronchial hyperreactivity in guinea pigs after orally bioavailable administration at 1 and 10 micrograms/kg, respectively. E6123 inhibited the PAF-induced increase in intracellular free calcium ion concentration ([Ca2+]i) in guinea pig eosinophils with an IC50 of 14 nM. References: Gundemir S, Johnson GV. Intracellular localization and conformational state of transglutaminase 2: implications for cell death. PLoS One. 2009 Jul 1;4(7):e6123. doi: 10.1371/journal.pone.0006123. PubMed PMID: 19568436; PubMed Central PMCID: PMC2701606.

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CAS：131614-02-3