產品名稱：SB 225002
產品貨號：LC  S-5100
產品規格：100 MG
SB 225002 is a potent and selective CXCR2 antagonist.  It inhibited IL-8 binding to CXCR2 with an IC50 of 22 nM.  SB 225002 showed >150-fold selectivity over CXCR1 and four other seven-transmembrane receptors tested.  SB 225002 potently inhibited human and rabbit neutrophil chemotaxis induced by both IL-8 and GROα in vitro and IL-8-induced rabbit neutrophil margination in vivo.  White, J.R., et al.  "Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration."  J. Biol. Chem. 273:  10095-10098 (1998).
SB 225002 significantly inhibited replication of HIV-1BRU in peripheral blood lymphocytes and of HIV-1BaL in monocyte-derived macrophages.  Lane, B.R., et al.  "Interleukin-8 stimulates human immunodeficiency virus type 1 replication and is a potential new target for antiretroviral therapy."  J. Virol. 75:  8195-8202 (2001).
SB 225002 indirectly inhibited gamma-secretase and reduced amyloid β.  It has the potential to be used to treat Alzheimer's disease.  Bakshi, P., et al.  "Structural optimization of a CXCR2-directed antagonist that indirectly inhibits gamma-secretase and reduces Abeta."  Bioorg. Med. Chem. 17:  8102-8112 (2009).
Growth-related oncogenes GROα, GROβ, and CXCR2 were up-regulated in esophageal tumor tissue.  SB 225002 intervened in GROα-CXCR2 and GROβ-CXCR2 signaling and inhibited esophageal tumorigenesis.  Wang, B., et al.  "A growth-related oncogene/CXC chemokine receptor 2 autocrine loop contributes to cellular proliferation in esophageal cancer."  Cancer Res. 66:  3071-3077 (2006).
After infection with S. pneumoniae, SB 225002 inhibited alveolar neutrophil and exudate macrophage recruitment in mice and led to increased lung bacterial loads.  Herbold, W., et al.  "Importance of CXC chemokine receptor 2 in alveolar neutrophil and exudate macrophage recruitment in response to pneumococcal lung infection."  Infect. Immun. 78:  2620-2630 (2010).
SB 225002 had inhibitory effects on both acute and chronic pain.  Manjavachi, M.N., et al.  "The effects of the selective and non-peptide CXCR2 receptor antagonist SB225002 on acute and long-lasting models of nociception in mice."  Eur. J. Pain 14:  23-31 (2010).
SB 225002 ameliorated 2,4,6-trinitrobenzene sulfonic acid-induced experimental colitis in mice.  Bento, A.F., et al.  "The selective nonpeptide CXCR2 antagonist SB225002 ameliorates acute experimental colitis in mice."  J. Leukoc. Biol. 84:  1213-1221 (2008).
Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

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