LIT-927 - CXCR - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELIT-927Cat. No.: HY-112709CAS No.: 2172879-52-4分式: CHClNO分量: 328.75作靶点: CXCR作通路: GPCR/G Protein; Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 12.5 mg/mL (38.02 mM;

2、 Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 1.25 mg/mL (3.80 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE物活性 LIT-927局部的、有服活性的 CXC 趋化因12 (CXCL12) 的中性配体，具有抗炎作，对 CXCL12 结合到其受体 CXCR4 的 Ki 值为 267 nM。IC50 & Target Ki: 267 nM (CXCL12) 1.体外研

3、究 LIT-927 is a locally and orally active CXCL12 neutraligand with anti-inflammatory effect, with a Ki of 267 nM forCXCL12 binding to CXCR4. Compounds 50, 57 (LIT-927), 65, and 67 are the most potent and soluble cyclicneutraligands identified in vitro and are representative of four novel chemotypes:

4、pyrazoline, pyrimidinone,benzofuranone, and chromanone. LIT-927 is bound to a wide and accessible pocket, which is incompatiblewith the observed nanomolar binding affinities of our neutraligands 1.体内研究 LIT-927 (compound 57) reduces eosinophil recruitment in a murine model of allergic airway hypereos

5、inophilia,LIT-927 is the only one to display inhibitory activity following oral administration. Combined with a high bindingselectivity for CXCL12 over other chemokines, LIT-927 represents a powerful pharmacological tool toinvestigate CXCL12 physiology in vivo and to explore the activity of chemokin

6、e neutralization in inflammatoryand related diseases 1.REFERENCES1. Regenass P, et al. Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a MurineModel of Allergic Airway Hypereosinophilia. J Med Chem. 2018 Sep 13;61(17):7671-7686.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400