CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
CXCR2 plays an important role in the activation and recruitment of neutrophils to sites of inflammation. CXCR2-IN-1 shows favorable central nervous system penetration property (Br/Bl>0.45)[1].
CXCR2-IN-1 shows efficacy in a cuprizone-induced demyelination model through oral administration, providing evidence to support CXCR2 to be a potential therapeutic target to treat demyelinating diseases such as multiple sclerosis[1].
[1]. Xu H, et al. Discovery of CNS Penetrant CXCR2 Antagonists for the Potential Treatment of CNS Demyelinating Disorders. ACS Med Chem Lett. 2016 Feb 8;7(4):397-402.