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Category:
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7TM Receptors Chemokine Receptors CXCR
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Cat.No.
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Product Name
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2725 |
SB 225002
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Price and Availability
Click here for full price details of
SB 225002
Other Information:
Sold for research purposes under agreement from
GlaxoSmithKline
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Chemical Name:
N-(2-Bromophenyl)-N'-(2-hydroxy-4-nitrophenyl)urea |
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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 mobilisation 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.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
White et al
(1998) Identification of a potent, selective non-peptide CXCR2 antagonist that
inhibits interleukin-8-induced neutrophil migration. J.Biol.Chem. 273
10095. Lane et al (2001) Interleukin-8 stimulates human
immunodeficiency virus type 1 replication and is a potential new target for
antiretroviral therapy. J.Virol. 75 8195. Catusse et al
(2003) Characterization of the molecular interactions of interleukin-8 (CXCL8),
growth related oncogen α
(CXCL1) and a non-peptide antagonist (SB 225002) with the human CXCR2.
Biochem.Pharmacol. 65 813.
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Keywords: SB 225002, Chemokine Receptors, Potent & Selective CXCR2 Antagonist, SB225002, Tocris Bioscience
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