cxcr2 antagonist 6

CXCR2 antagonist 6 (compound 35c) 是一种有效的CXCR2拮抗剂。CXCR2 antagonist 6 显示出有效的CXCR2结合亲和力 (IC50=0.43 μM) 和钙动员 (IC50=0.11 μM)。

CXCR2/CCR7 antagonist-1 (compound 6) 是高效的CXCR2和CCR7双重拮抗剂，其IC50值分别为0.0046和0.0014 μM。此化合物适用于肿瘤转移及自身免疫性疾病的研究。

(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-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1]. CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in rat and mouse air pouch models[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.