688763-64-6

688763-64-6 structure

Name: Elubrixin
Chemical Name: 1-(2-chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea
CAS Number: 688763-64-6
Molecular Formula: C₁₇H₁₇Cl₂FN₄O₄S
Molecular Weight: 463.31100
Catalog: Signaling Pathways GPCR/G Protein CXCR
Create Date: 2016-12-29 07:11:35
Modify Date: 2024-01-08 15:13:43
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation[1][2][3].

Name	1-(2-chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea
Synonyms	Elubrixin UNII-MW2AIJ8USP

Description	Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin can be used for inflammatory diseases such as inflammatory bowel disease and airway inflammation[1][2][3].
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Interleukin Related Signaling Pathways >> GPCR/G Protein >> CXCR Research Areas >> Inflammation/Immunology Signaling Pathways >> Immunology/Inflammation >> CXCR
Target	CXCR2[2][3] IL-8 receptor[1]
In Vitro	Elubrixin has an inhibitory effect on neutrophils in a dose-dependent fashion[1].
References	[1]. Mozaffari S, et al. Inflammatory bowel disease therapies discontinued between 2009 and 2014. Expert Opin Investig Drugs. 2015;24(7):949-56. [2]. Lazaar AL, et al. SB-656933, a novel CXCR2 selective antagonist, inhibits ex vivo neutrophil activation and ozone-induced airway inflammation in humans. Br J Clin Pharmacol. 2011 Aug;72(2):282-93. [3]. Nicholson GC, et al. A novel flow cytometric assay of human whole blood neutrophil and monocyte CD11b levels: upregulation by chemokines is related to receptor expression, comparison with neutrophil shape change, and effects of a chemokine receptor (CXCR2) antagonist. Pulm Pharmacol Ther. 2007;20(1):52-9.

Hazard Codes	Xi