cx3cr1

AZD8797 (KAND567) 是一种可口服且具有选择性和有效性的人 CX3CR1 变构拮抗剂，对 CX3CR1 和 CXCR2 具有抑制作用，对SARS-CoV-2诱导的神经元损伤有潜在的保护作用，可防止癫痫发作后偏头痛模型大鼠痛觉过敏和小胶质细胞活化的恶化。

E6130 may be effective in the treatment of inflammatory bowel disease and is a highly selective CX3CR1 regulator for oral administration.

JMS-17-2 是选择性CX3CR1拮抗剂(IC50:0.32 nM)，能够抑制乳腺癌细胞的转移和定植。

JMS-17-2 hydrochloride, a highly potent and selective CX3CR1 antagonist with an IC 50 value of 0.32 nM, effectively impedes the metastatic seeding and colonization process of breast cancer cells.

Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectively.

TREM2-IN-1 (OPA) 是一种铂类 TREM2 抑制剂，具有抗癌抗肿瘤活性，通过阻止 DNA 复制和抑制髓样细胞 2 （TREM2） 上表达的触发受体发挥作用。TREM2-IN-1 抑制巨噬细胞上 TREM2 的免疫调节活性，通过减少 CD206 和 CX 的数量来阻止携带 MC38 结直肠肿瘤的小鼠模型的肿瘤生长+3CR1 免疫抑制性巨噬细胞。