cxcr1

Reparixin (Repertaxin) 是两种 CXCL8 受体 CXCR1 2 的强效抑制剂，它对 CXCR2 介导的细胞迁移具有微弱的抑制作用 ，IC50为 100 nM。它强烈阻断 CXCR1 介导的趋化性，IC50为 1 nM。

SX-682 是口服有效的 CXCR1和 CXCR2变构抑制剂，可以阻断肿瘤髓系抑制细胞募集并增强 T 细胞活化和抗肿瘤免疫，具有治疗去势抵抗性前列腺癌的潜力。

Navarixin (MK-7123) 是一种可口服的 CXCR1和 CXCR2变构拮抗剂，对猕猴 CXCR1的 Kd 值为 41 nM，对大小鼠和猕猴 CXCR2的 Kd 值分别为 0.20、0.20 和 0.08 nM。

Delmetacin (Demethacin) 是一种非甾体抗炎化合物，具有抗炎和镇痛活性，对 CXC 趋化因子受体 CXCR1 具有抑制作用。

SCH 563705 是一种可口服且具有高效性的 CXCR2 和 CXCR1 拮抗剂，可用于研究急性呼吸综合征、慢性阻塞性肺病和炎症。

CXCL-CXCR1 2-IN-1 是一种具有口服活性哈和高效性的 ELR+CXCL-CXCR1 2 通路抑制剂，具有抗癌和抗血管生成活性，可用于研究心血管疾病和癌症。

Reparixin L-lysine salt (Repertaxin L-lysine salt) 是趋化因子受体1 2 活化的变构抑制剂。

SX-517 is a potent noncompetitive boronic acid CXCR1 2 antagonist. SX-517 inhibits CXCL1-induced Ca(2+) flux (IC50 = 38 nM) in human PMNs.

Ladarixin is a dual, non-competitive allosteric inhibitor of CXCR1 and CXCR2 interleukin8 (IL-8a and IL-8b, respectively). The efficacy of CXCR1 2 inhibition prevents inflammation and autoimmune-mediated islet damage.

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.

SX-576 is undergoing further investigation as a potential therapy for pulmonary inflammation. It is also a potent non-competitive boronic acid-containing CXCR1 2 antagonists.