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About This Item
Empirical Formula (Hill Notation):
C13H10BrN3O4
CAS Number:
Molecular Weight:
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
Quality Level
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
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
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)
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Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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Global Trade Item Number
| SKU | GTIN |
|---|---|
| 559405-1MG | 04055977191967 |