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Chemokine (C-C motif) receptor 4 (CCR4) antagonist is an antagonist of CCR4.1 It inhibits activation of CCR4 by chemokine (C-C motif) ligand 22 (CCL22) in a [35S]GTPγS assay and also inhibits chemotaxis in human and mouse CCR4-expressing B300-19 cells (IC50s = 18, 140, and 39 nM, respectively). CCR4 antagonist inhibits microglial activation in the cortex in a mouse model of hepatic encephalopathy induced by the neurotoxin azoxymethane when administered at a dose of 1 mg/kg per day.2 It reduces azoxymethane-induced increases in Il6 and Il1b expression in mouse cortex. CCR4 antagonist reduces mechanical and thermal sensitivity in a mouse model of type I diabetes induced by streptozotocin (Item No. 13104) when administered intrathecally at doses ranging from 10 to 30 µg/animal.3
WARNING This product is not for human or veterinary use.
1. Discovery of potent CCR4 antagonists: Synthesis and structure-
2. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J. Neuroinflammation 11, 121 (2014).
3. Blockade of CCR4 diminishes hypersensitivity and enhances opioid analgesia -