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LIT-927

Chemical Structure : LIT-927

CAS No.: 2172879-52-4

LIT-927 (LIT927)

Catalog No.: PC-35600Not For Human Use, Lab Use Only.

LIT-927 (LIT927) is the first selective, locally and orally active CXCL12 neutraligand with Ki of 267 nM for CXCL12-TR binding inhibition.

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Biological Activity

LIT-927 (LIT927) is the first selective, locally and orally active CXCL12 neutraligand with Ki of 267 nM for CXCL12-TR binding inhibition; displays excellent selectivity over other chemokines (CCL17, CCL22, CCL5 and CCL2), inhibits the increase in intracellular calcium concentration in EGFP-CXCR4+HEK cells in response to CXCL12 at 10 uM, has no effect on calcium responses triggered by either CCL17 or CCL22 on EGFP-CCR4+HEK cells, CCL5 on EGFP-CCR5+ HEK cells, or by CCL2 on EGFP-CCR2+HEK cells; reduces eosinophil recruitment in murine model of allergic airway hypereosinophilia.

Physicochemical Properties

M.Wt 328.752
Formula C17H13ClN2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(4-Chlorophenyl)-6-(4-hydroxy-3-methoxyphenyl)pyrimidin-2(1H)-one

References

1. Regenass P, et al. J Med Chem. 2018 Aug 28. doi: 10.1021/acs.jmedchem.8b00657.

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