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LIT-927
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CAS NO:2172879-52-4
规格:98%
分子量:328.75
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍

LIT-927

LIT-927 is a locally and orally active CXCL12 neutraligand
CAS:2172879-52-4
分子式:C??H??ClN?O?
分子量:328.75
纯度:98%
存储:Store at -20°C

Background:

LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12 binding to its specific receptor CXCR4[1] .


LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM for CXCL12 binding to CXCR4. 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].


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].


Reference:


[1]. Regenass P, et al. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia. J Med Chem. 2018 Sep 13;61(17):7671-7686.