|1-(2-溴苯基)-3-(2-羟基-4-硝基苯基)脲|CsnPharm

CAS No.: 182498-32-4

SB225002 Catalog No. CSN17197

Synonyms: N/A

SB225002 is a potent and selective non-peptide inhibitor of CXCR2 with IC50 of 22 nM, showing > 150-fold selectivity over CXCR1 and four other 7-TMRs.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 CXCR2

IC50:22nM
描述CXCR2 is expressed in human neutrophilsand a subset of T-cells, which can mediate neutrophil migration to sites of inflammation through binding with and internalization through its ligand IL-8 or related chemokines containing a common amino-terminal ELR amino acid sequence (Glu-Leu-Arg), such as GROα, GROβ, GROγ, NAP-2 and ENA-78. SB 225002 is a non-peptide, potent and selective CXCR2 inhibitor with IC50 value of 22 nM, >150-fold selectivity over CXCR1 and four other 7-TMRs tested. SB-225002 can produce a dose-dependent inhibition of calcium mobilization induced by IL-8 and GROα with IC50 values of 8 nM and 10 nM, respectively, in differentiated HL60 cells with predominantly express CXCR2 (80%) with a much smaller number of CXCR1 (20%) receptors, as well as inhibit both IL-8 (1nM)- and GROα (10nM)-mediated human neutrophil chemotaxis with IC50s of 20 nM and 60 nM, respectively. This effect of SB-225002 on chemotaxis can also be observed in in vivo study^[1]. Daily intraperitoneal injection with SB225002 at dose of 5 mg/kg for 4 weeks showed significantly tumor growth inhibition by ~45% decrease in tumor size of LLC tumor bearing GRK6-/- mice.
作用机制SB-225002 can inhibit CXCR2 through competition with IL-8.^[1]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
CHO cells	-	Function assay	-	Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells, IC50=22 nM	17236763
HEK293 cells	-	Function assay	-	Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=40 nM	25254640
human PMNs	-	Function assay	-	Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay, IC50=30 nM	25254640

动物研究
剂量
Mice: 0.3 mg/kg - 1 mg/kg^[3] (i.p.), 4 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Mice: 0.3 mg/kg - 1 mg/kg^[3] (i.p.), 4 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] White JR, Lee JM, et al. Identification of a potent, selective non-peptide CXCR2 antagonist that inhibits interleukin-8-induced neutrophil migration. J Biol Chem. 1998 Apr 24;273(17):10095-8.
[2] Raghuwanshi SK, Smith N, et al. G protein-coupled receptor kinase 6 deficiency promotes angiogenesis, tumor progression, and metastasis. J Immunol. 2013 May 15;190(10):5329-36.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8398 mL
- 14.1989 mL
- 28.3978 mL
- 5 mM
- 0.5680 mL
- 2.8398 mL
- 5.6796 mL
- 10 mM
- 0.2840 mL
- 1.4199 mL
- 2.8398 mL

技术信息

CAS号

182498-32-4

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H10BrN3O4

运输

蓝冰

分子量

352.14

别名

N/A

溶解度

DMSO	460.0 mg/mL (1306.3 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+35% PEG300+water	2.5 mg/mL	clear
PO	0.5% CMC-Na	41 mg/mL	suspension

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SB225002 Catalog No. CSN17197

靶点选择性

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