LIT-927 is an orally bioavailable neutraligand that binds to chemokine (C-X-C motif) ligand 12 (CXCL12; K = 267 nM in a FRET-based binding assay). It is selective for inhibiting calcium accumulation induced by CXCL12 over that induced by chemokine (C-C motif) ligand 17 (CCL17), CCL22, CCL5, and CCL2 at 10 µM. It inhibits pulmonary artery smooth muscle cell and pericyte migration in vitro. LIT-927 (100 mg/kg per day) inhibits increases in serum levels of CXCL12, as well as reduces total pulmonary vascular resistance and remodeling of pulmonary arterioles, in a rat model of pulmonary hypertension induced by monocrotaline . It inhibits allergen-induced eosinophil infiltration into the lung by 62% in a mouse model of allergic airway hypereosinophilia when administered at an oral dose of 1,400 µmol/kg.