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LIT-927 is a novel CXCL12 neutral ligand that inhibits the binding of CXCL12 to Texas red dye with a Ki value of 267 nM. It is highly selective to CXCL12.
Brand: BCM
Target: CXCR
Signaling Pathways: Autophagy; GPCR/G Protein; Immunology/Inflammation
In Vitro: LIT-927 at 10 μM is able to inhibit the increase in intracellular calcium concentration in EGFP-CXCR4+ HEK cells in response to CXCL12, while it has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+ HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or CCL2 on EGFPCCR2+ HEK cells.
In Vivo: LIT-927 (350 μmol/kg) inhibited eosinophil infiltration by 54% and 55%. LIT-927 did not exhibit any side effects. In the same murine model of hypereosinophilia, LIT-927 (1400 μmol/kg, P.O.) shows a large and statistically reliable inhibition of eosinophil recruitment (62% inhibition).
Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.
Isomeric SMILES: COC1=C(C=CC(=C1)C2=NC(=O)NC(=C2)C3=CC=C(C=C3)Cl)O
InChIKey: BYYRNPIGDRRGLJ-UHFFFAOYSA-N
InChI: 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)
Attribute [Chem Name] 6-(4-chlorophenyl)-4-(4-hydroxy-3-methoxyphenyl)-1H-pyrimidin-2-one [CAS No.] 2172879-52-4 [MDL No.] MFCD31726172 [Formula] C17H13ClN2O3 [Molecular] 328.75 [Form] A solid [Storage] Sealed in dry. Stored at -20°C.
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