cxcr2-in-2

(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(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)。

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

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。

Ladarixin (DF 2156A free base) is an orally active, non-competitive CXCR1/CXCR2 allosteric inhibitor that suppresses AKT, NF-κB, and angiogenesis, thereby slowing the progression of experimental human melanoma. It may be employed in research concerning COPD, asthma, and melanoma.

CXCR2 antagonist 3 (compound 11h) is a highly effective antagonist of CXC chemokine receptor 2 (CXCR2). It displays potent activity in inhibiting neutrophil infiltration into the air pouch, with double-digit nanomolar potencies against CXCR2. Moreover, CXCR2 antagonist 3 reduces the infiltration of neutrophils and MDSCs, while enhancing the infiltration of CD3+ T lymphocytes into Pan02 tumor tissues [1].

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。

Corydalmine hydrochloride 抑制某些植物病原体的孢子萌发以及腐生真菌。Corydalmine hydrochloride 具有口服活性，可用于缓解疼痛的研究。Corydalmine hydrochloride 通过抑制 NF-κB 依赖性的 CXCL1/CXCR2信号传导途径，可缓解 Vincristine 引起的神经性疼痛。