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The purpose of this study was to characterize the neuroprotective and neurotrophic effect of a novel CXCR4 antagonist CX549. We demonstrated that CX549 had a higher affinity for CXCR4 and was more potent than AMD3100 to inhibit CXCL12-mediated chemotaxis in culture. CX549 effectively reduced the activation of microglia and improved neuronal survival after injury in neuron\/microglia cocultures. Early poststroke treatment with CX549 significantly improved behavioral function, reduced brain infarction, and suppressed the expression of inflammatory markers. Compared to AMD3100, CX549 has a higher affinity for CXCR4, is more efficient to mobilize HSCs for transplantation, and induces behavioral improvement. Our data support that CX549 is a potent anti-inflammatory agent, is neuroprotective against ischemic brain injury, and may have clinical implications for the treatment of stroke.<\/jats:p>","DOI":"10.3727\/096368916x693563","type":"journal-article","created":{"date-parts":[[2017,4,12]],"date-time":"2017-04-12T23:03:11Z","timestamp":1492038191000},"page":"571-583","update-policy":"https:\/\/doi.org\/10.1177\/sage-journals-update-policy","source":"Crossref","is-referenced-by-count":30,"title":["A Novel CXCR4 Antagonist CX549 Induces Neuroprotection in Stroke Brain"],"prefix":"10.1177","volume":"26","author":[{"given":"Kuo-Jen","family":"Wu","sequence":"first","affiliation":[{"name":"Center for Neuropsychiatric Research, National Health Research Institutes (NHRI), Miaoli, Taiwan"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Seong-Jin","family":"Yu","sequence":"additional","affiliation":[{"name":"Center for Neuropsychiatric Research, National Health Research Institutes 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