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).

• Sinônimo(s): SB 225002, N-(2-Hydroxy-4-nitrophenyl)-Nʹ-(2-bromophenyl)urea, CXCR2 Antagonist II
• Fórmula empírica (Notação de Hill): C₁₃H₁₀BrN₃O₄
• Número CAS: 182498-32-4
• Peso molecular: 352.14
• Código UNSPSC: 51111800
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• forma: solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: yellow
• solubilidade: DMSO: 200 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: −20°C
• 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)
• chave InChI: MQBZVUNNWUIPMK-UHFFFAOYSA-N

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Outras notas

Bakshi, P., et al. 2009. ACS Chem. Biol.in press.
White, J.R., et al. 1998. J. Biol. Chem. 273, 10095.

Informações legais

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable