cxcr2 in 2

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.

(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 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].

NVP CXCR2 20 is an effective selective CXCR2 antagonist (IC50 = 40 nM) with oral bioavailability.

CXCR2 antagonist 8 是可用于研究胰岛素抵抗的，CXCR2受体的选择性拮抗剂。

CXCR2 antagonist 5 (compound 25) 是一种有效的CXCR2拮抗剂。 CXCR2 antagonist 5 显示出有效的CXCR2结合亲和力 (IC50=0.013 μM) 和钙动员 (IC50=0.1 μM)。

CXCR2 antagonist 7 (compound 19) 是一种有效的CXCR2拮抗剂。CXCR2 antagonist 7 显示出有效的CXCR2结合亲和力 (IC50=0.044 μM) 和钙动员 (IC50=0.66 μM)。

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 antagonist 2 是一种有效的癌症免疫治疗的 CXCR2拮抗剂，IC50值为 95 nM。

CXCR2 antagonist 4 (compound 7) is a highly potent antagonist that inhibits CXCR2 with an IC50 value of 0.13 μM. It also effectively inhibits the cytosolic calcium increase induced by CXCL8, with an IC50 value of 27 μM. CXCR2 antagonist 4 shows promising potential for anticancer research [1].

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

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。

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。

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。