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).

• Szinonimák: SB 225002, N-(2-Hydroxy-4-nitrophenyl)-Nʹ-(2-bromophenyl)urea, CXCR2 Antagonist II
• Tapasztalati képlet (Hill-képlet): C₁₃H₁₀BrN₃O₄
• CAS-szám: 182498-32-4
• Molekulatömeg: 352.14
• MDL-szám: MFCD00954637
• UNSPSC kód: 51111800
• NACRES: NA.77

Tulajdonságok

• Minőségi szint: 100
• Teszt: ≥95% (HPLC)
• Forma: solid
• gyártó/kereskedő neve: Calbiochem^®
• tárolási körülmény: OK to freeze; protect from light
• szín: yellow
• oldhatóság: DMSO: 200 mg/mL
• kiszállítva: ambient
• tárolási hőmérséklet: −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)
• Nemzetközi kémiai azonosító kulcs: MQBZVUNNWUIPMK-UHFFFAOYSA-N

Leírás

Általános leírás

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.

Biokémiai/fiziológiai hatások

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

Kiszerelés

Packaged under inert gas

Figyelmeztetés

Toxicity: Standard Handling (A)

Egyéb megjegyzések

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

Jogi információk

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

Biztonsági adatok

• Tárolási osztály kódja: 11 - Combustible Solids
• WGK: WGK 3
• Lobbanási pont (F): Not applicable
• Lobbanási pont (C): Not applicable