Description
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrationsIn VitroML604086 (0-100 µM) inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations of cell lines stably expressing cyno CCR8 with IC 50 s of 1.3 µM and 1.0 µM, respectively. ML604086 (10, 30 µM; 64 h) inhibits CCL1 binding to CCR8 on CD4 T-cells, and inhibits the serotonin receptor 5HT1a with the inhibition rate of 30%, 70% at 10, 30 µM respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoML604086 (1.038 mg/kg; intravenous infusion) shows no effect on airway eosinophilia, pro-inflammatory cytokine production or airway resistance and compliance in Macaca fascicularis. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 3.0-5.0 kg male and female adult Macaca fascicularis (primate model\nof asthma)Dosage: 1.038 mg/kg Administration: Intravenous infusion Result: Did not effected the Changes in airway resistance and compliance induced by allergen provocation and increasing concentrations of methacholine.Form:SolidIC50& Target:CCR8