LIT-927

LIT-927 is an orally bioavailable neutraligand that binds to chemokine (C-X-C motif) ligand 12 (CXCL12, Ki = 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 (Cay-16666). 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.Formal Name: 4-(4-chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)-2(1H)-pyrimidinone. CAS Number: 2172879-52-4. Molecular Formula: C17H13ClN2O3. Formula Weight: 328.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 1mg/mL. lambdamax: 263, 365 nm. SMILES: OC1=C(OC)C=C(C(N2)=CC(C3=CC=C(Cl)C=C3)=NC2=O)C=C1. InChi Code: InChI=1S/C17H13ClN2O3/c1-23-16-8-11(4-7-15(16)21)14-9-13(19-17(22)20-14)10-2-5-12(18)6-3-10/h2-9,21H,1H3,(H,19,20,22). InChi Key: BYYRNPIGDRRGLJ-UHFFFAOYSA-N.