LIT927

Cas No.:	2172879-52-4
Chemical Name:	4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)pyrimidin-2(1H)-one
Synonyms:	LIT927,LIT-927,LIT 927
SMILES:	O=C1N=C(C2=CC=C(Cl)C=C2)C=C(C3=CC=C(O)C(OC)=C3)N1
Formula:	C17H13ClN2O3
M.Wt:	328.752
Sotrage:	2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO

Description:	LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding.
In Vivo:	LIT-927 (compound 57) reduces eosinophil recruitment in a murine model of allergic airway hypereosinophilia, LIT-927 is the only one to display inhibitory activity following oral administration. Combined with a high binding selectivity for CXCL12 over other chemokines, 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[1].
In Vitro:	LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12-TR binding. Compounds 50, 57 (LIT-927), 65, and 67 are the most potent and soluble cyclic neutraligands identified in vitro and are representative of four novel chemotypes: pyrazoline, pyrimidinone, benzofuranone, and chromanone. LIT-927 is bound to a wide and accessible pocket, which is incompatible with the observed nanomolar binding affinities of our neutraligands[1].