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960495-43-6

960495-43-6 structure
960495-43-6 structure
  • Name: Elubrixin tosylate
  • Chemical Name: 1-(2-chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea,4-methylbenzenesulfonic acid
  • CAS Number: 960495-43-6
  • Molecular Formula: C24H25Cl2FN4O7S2
  • Molecular Weight: 635.51200
  • Catalog: Signaling Pathways GPCR/G Protein CXCR
  • Create Date: 2016-06-20 00:34:50
  • Modify Date: 2024-01-16 17:13:42
  • 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].

Name 1-(2-chloro-3-fluorophenyl)-3-(4-chloro-2-hydroxy-3-piperazin-1-ylsulfonylphenyl)urea,4-methylbenzenesulfonic acid
Synonyms UNII-13FVR7WD4P
Elubrixin tosylate
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
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.

Molecular Formula C24H25Cl2FN4O7S2
Molecular Weight 635.51200
Exact Mass 634.05300
PSA 185.39000
LogP 6.83260

~%

960495-43-6 structure

960495-43-6

Literature: SMITHKLINE BEECHAM CORPORATION Patent: WO2007/150015 A2, 2007 ; Location in patent: Page/Page column 10-11 ; WO 2007/150015 A2