| Bioactivity | CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonist with a pIC50 of 9.3. | ||||||||||||
| Invitro | CXCR2 plays an important role in the activation and recruitment of neutrophils to sites of inflammation. CXCR2-IN-1 (compound 22) shows favorable central nervous system penetration property (Br/Bl>0.45)[1]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | CXCR2-IN-1 | ||||||||||||
| CAS | 1873376-49-8 | ||||||||||||
| Formula | C19H20Cl2FN3O4S | ||||||||||||
| Molar Mass | 476.35 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |