cxcr2 in 1

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

AZ10397767 is a potent CXCR2 antagonist (IC50 = 1 nM). AZ10397767 significantly reduced the numbers of infiltrating neutrophils into both in vitro and in vivo tumor models.

Nicotinamide N-oxide (Nicotinamide 1-oxide) 是生物体内烟酰胺分解代谢物，是高效选择性CXCR2受体拮抗剂。

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。

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。

(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.

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].

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。