LIT-927

Description: LIT-927 is a novel potent, locally and orally bioactive neutraligand for the chemokine CXCL12 with a Ki of 267 nM for CXCL12-TR binding. It has anti-inflammatory effect in a murine model of allergic airway hypereosinophilia. LIT-927 binds the chemokine CXCL12, not its cognate receptors CXCR4 or CXCR7, and neutralizes its biological activity. LIT-927 is a novel neutraligand of CXCL12 which displays a higher solubility than the lead compound and is no longer a Michael acceptor. LIT-927 reduces eosinophil recruitment in a murine model of allergic airway hypereosinophilia, LIT-927 represents a powerful pharmacological tool to investigate CXCL12 physiology in vivo and to explore the activity of chemokine neutralization in inflammatory and related diseases.

References: J Med Chem. 2018 Sep 13; 61(17):7671-7686.