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Cat. No. Product Name Target Signaling Pathways
T36923 CXCR2-IN-2

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 ra...
T10905 CXCR2-IN-1

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
CXCR2-IN-1是可渗透中枢神经系统的 CXCR2拮抗剂,pIC50值为9.3。
T36443 (R,R)-CXCR2-IN-2

(R,R)-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.
T7130 Navarixin

MK-7123,SCH 527123

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
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。
T14384 AZD8797

KAN-0440567,KAND567

CXCR Autophagy; GPCR/G Protein; Immunology/Inflammation
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。
T61356 CXCR2 antagonist 3

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].
T75642 Corydalmine hydrochloride

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。

化合物

CXCR2-IN-2
Cat.No: T36923
Synonym: CXCR2-IN-2
Target:
CXCR2-IN-1
Cat.No: T10905
Synonym:
Target: CXCR
(R,R)-CXCR2-IN-2
Cat.No: T36443
Synonym: (R,R)-CXCR2-IN-2
Target:
Navarixin
Cat.No: T7130
Synonym: MK-7123,SCH 527123
Target: CXCR
AZD8797
Cat.No: T14384
Synonym: KAN-0440567,KAND567
Target: CXCR
CXCR2 antagonist 3
Cat.No: T61356
Synonym:
Target:
Corydalmine hydrochloride
Cat.No: T75642
Synonym:
Target:
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