Description: Potent and selective CXCR2 antagonist
Chemical Name:N-(2-Bromophenyl)-N'-(2-hydroxy-4-nitrophenyl)urea
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent and selective CXCR2 chemokine receptor antagonist (IC50 = 22 nM) that displays > 150-fold selectivity over CXCR1 receptors. Causes inhibition of IL-8 and GROα-mediated calcium mobilization in HL60 cells (IC50 values are 8 and 10 nM respectively). Prevents IL-8-induced neutrophil chemotaxis in vitro and sequestration in vivo. Inhibits HIV replication in lymphocytes and macrophages.
Licensing Information
Sold for research purposes under agreement from GlaxoSmithKline
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Technical Data
M. Wt
352.14
Formula
C13H10BrN3O4
Storage
Store at RT
Purity
≥99% (HPLC)
CAS Number
182498-32-4
PubChem ID
3854666
InChI Key
MQBZVUNNWUIPMK-UHFFFAOYSA-N
Smiles
OC1=CC(=CC=C1NC(=O)NC1=CC=CC=C1Br)[N+]([O-])=O
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent
Max Conc. mg/mL
Max Conc. mM
Solubility
DMSO
35.21
100
ethanol
17.61
50
Preparing Stock Solutions
The following data is based on the product molecular weight 352.14. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass
1 mg
5 mg
10 mg
1 mM
2.84 mL
14.2 mL
28.4 mL
5 mM
0.57 mL
2.84 mL
5.68 mL
10 mM
0.28 mL
1.42 mL
2.84 mL
50 mM
0.06 mL
0.28 mL
0.57 mL
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Whiteet al (1998) Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J.Biol.Chem. 273 10095 PMID: 9553055
Laneet al (2001) Interleukin-8 stimulates human immunodeficiency virus type 1 replication and is a potential new target for antiretroviral therapy. J.Virol. 75 8195 PMID: 11483765
Catusseet al (2003) Characterization of the molecular interactions of interleukin-8 (CXCL8), growth related oncogen a (CXCL1) and a non-peptide antagonist (SB 225002) with the human CXCR2. Biochem.Pharmacol. 65 813 PMID: 12628493