559405
SB 225002
A potent, selective, and competitive antagonist of the G-protein coupled receptor CXCR2 (IL-8RB; IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2).
别名:
SB 225002, N-(2-Hydroxy-4-nitrophenyl)-Nʹ-(2-bromophenyl)urea, CXCR2 Antagonist II
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关于此项目
经验公式（希尔记法）:
C13H10BrN3O4
化学文摘社编号:
分子量:
352.14
MDL number:
UNSPSC Code:
51111800
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light
SMILES string
Brc1c(cccc1)NC(=O)Nc2c(cc(cc2)[N+](=O)[O-])O
InChI
1S/C13H10BrN3O4/c14-9-3-1-2-4-10(9)15-13(19)16-11-6-5-8(17(20)21)7-12(11)18/h1-7,18H,(H2,15,16,19)
InChI key
MQBZVUNNWUIPMK-UHFFFAOYSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
−20°C
Quality Level
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General description
A potent and selective antagonist of G-protein coupled receptor CXCR2 (IL-8RB; IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2). Inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROα in vitro and selectively blocks IL-8-induced neutrophil margination in rabbits. Reduces presenilin expression, inhibits γ-secretase activity, and blocks Aβ40/42 production and notch processing; further, demonstrates in vivo efficacy in mouse models.
A potent, selective, and competitive antagonist of the G-protein coupled receptor CXCR2 (IL-8RB; IC50 = 22 nM for the inhibition of 125I-IL-8 binding to CXCR2). Shows ~150-fold selectivity over CXCR1. Inhibits human and rabbit neutrophil chemotaxis induced by both IL-8 and GROα in vitro and in vivo selectively blocks IL-8-induced neutrophil margination in rabbits. Reduces presenilin expression, inhibits γ-secretase activity, and blocks Aβ40/42 production and notch processing; further, demonstrates in vivo efficacy in mouse models.
Biochem/physiol Actions
Cell permeable: no
Product does not compete with ATP.
Reversible: no
Target IC50: 22 nM for the inhibition of 125I-IL-8 binding to CXCR2
Packaging
Packaged under inert gas
Other Notes
Bakshi, P., et al. 2009. ACS Chem. Biol.in press.
White, J.R., et al. 1998. J. Biol. Chem. 273, 10095.
White, J.R., et al. 1998. J. Biol. Chem. 273, 10095.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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