Name | LIT-927 |
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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. |
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Related Catalog | |
Target |
Ki: 267 nM (CXCL12-TR)[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]. |
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]. |
References |
Molecular Formula | C17H13ClN2O3 |
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Molecular Weight | 328.75 |
Storage condition | 2-8℃ |