CXCR拮抗剂;CXCR Antagonists;;InformationAZD5069 AZD5069 is a novel antagonist of CXCR2 , which is shown to inhibit binding of CXCL8 to CXCR2 with a pIC50 value of 8.8 and inhibit CXCL8 binding to CXCR1 with pIC50 values of 6.5.TargetsCXCR2In vitroAZD5069 is a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics.In vivoIn preclinical models, airway neutrophil recruitment in response to inflammatory challenge is abrogated by selective targeting of CXCR2 using AZD5069.
参考文献:
1. Norman P, et al. Evidence on the identity of the CXCR2 antagonist AZD-5069. Expert Opin Ther Pat. 2013 Jan;23(1):113-7.