Elubrixin tosylate

Names

[ Name ]:
Elubrixin tosylate

[Synonym ]:
UNII-13FVR7WD4P
Elubrixin tosylate

Biological Activity

[Description]:

Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, 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

IL-8

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₄H₂₅Cl₂FN₄O₇S₂

[ Molecular Weight ]:
635.51200

[ Exact Mass ]:
634.05300

[ PSA ]:
185.39000

[ LogP ]:
6.83260

Elubrixin tosylate

Names

Biological Activity

Chemical & Physical Properties

Synthetic Route

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Related Compounds