cxcr-2-in-2

CXCR2-IN-2(compound 68)是一种高度选择性的CXCR2拮抗剂(IC50=5.2nM)，具有可穿透血脑屏障和可口服的优点，能够抑制人全血Gro-α诱导的CD11b表达(IC50=0.04 μM)。

(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively[1]. [1]. Lu H, et al. Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists. J Med Chem. 2018;61(6):2518-2532.

CXCR2-IN-1是可渗透中枢神经系统的 CXCR2拮抗剂，pIC50值为9.3。