Cloricromen

Cloricromen (Cloricromene) is an orally active platelet inhibitor. Cloricromen inhibits thromboxane B₂ release, β-thromboglobulin, and thrombus formation. Cloricromen inhibits LPS (HY-D1056)-induced NF-κB activation, oxidative activity, and TNF-α expression. Cloricromen exhibits protective activity in animal models of shock and peripheral ischaemia. Cloricromen can be used for the research of myocardial ischaemia/reperfusion injury, and ischaemic cerebrovascular disease^[1][2][3][4]. In Vitro:Cloricromen (1-50 μM; 10 min pre-incubation before 24 h LPS exposure) potently inhibits lipopolysaccharide-induced TNF-α release in rat alveolar macrophages with an IC₅₀ of 5.9 μM, without inducing cytotoxicity^[3].
Cloricromen (10 μM; 10 min pre-incubation before 2 h LPS exposure) inhibits LPS-induced TNF-α mRNA expression in rat alveolar macrophages, indicating a pre-transcriptional mechanism of action^[3].
Cloricromen (1-50 μM; 10 min pre-incubation before 15 min LPS exposure) LPS-induced NF-κB activation in a dose-dependent manner in rat alveolar macrophages by targeting activation, not direct DNA binding^[3].
Cloricromen (10 μM; 10 min pre-incubation before 5 min LPS exposure) has only a slight effect on lipopolysaccharide-induced PKC-βII translocation in rat alveolar macrophages^[3].
Cloricromen (10 μM; 10 min pre-incubation before LPS exposure) significantly inhibits lipopolysaccharide-induced cellular oxidative activity in rat alveolar macrophages^[3]. In Vivo:Cloricromen (30-300 μg/kg/min; i.v.; continuous infusion; from 15 minutes pre-occlusion through 2-hour reperfusion) induces dose-dependent cardioprotection in rabbits with myocardial ischaemia-reperfusion injury^[1].
Cloricromene protects against LPS-induced endotoxic shock in male Sprague-Dawley rats by inhibiting TNF-α production, improving survival, and reversing associated hemodynamic and hematological abnormalities^[3].
Cloricromene reduces myocardial infarct size in male Sprague-Dawley rats subjected to ischemia-reperfusion injury^[3].
Cloricromene (0.25-0.50 mg/kg; i.v.; continuous infusion; up to 70 minutes) reduces myocardial ischemia-reperfusion injury in rabbits^[4].