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SB-265610

SB-265610用途

SB-265610 是一种选择性的竞争性非肽变构 CXCR2 拮抗剂。SB-265610 阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50 分别为 3.7 nM 和 70 nM。

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SB-265610名称

[ CAS 号 ]:
211096-49-0

[ 英文名 ]:
SB 265610

[英文别名 ]:

SB 265610

SB-265610生物活性

[ 描述 ]:

SB-265610 是一种选择性的竞争性非肽变构 CXCR2 拮抗剂。SB-265610 阻断大鼠 CINC-1 诱导的钙动员和中性粒细胞趋化性,IC50 分别为 3.7 nM 和 70 nM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> CXCR

研究领域 >> 炎症/免疫

信号通路 >> 免疫及炎症 >> CXCR

[ 靶点 ]

CXCR2

[体外研究]

在体外,SB-265610以浓度依赖性方式拮抗大鼠细胞因子诱导的中性粒细胞化学引诱物-1(CINC-1)诱导的钙动员,IC50为3.7nM,和大鼠中性粒细胞趋化性,IC50为70nM。SB-265610将CINC-1的抗细胞凋亡作用降低至未用CINC-1处理的水平[1]。

[体内研究]

在伤口修复过程中SB-265610(100mg/kg/天；口服给药；每日；5天；CXCR2野生型小鼠)治疗显着延迟CXCR2野生型小鼠的愈合参数[2]。动物模型：氮芥野生型小鼠[2]剂量：100 mg/kg/天给药：口服给药；每日；5天结果：伤口愈合过程明显受损。

[参考文献]

[1]. Auten RL, et al. Nonpeptide CXCR2 antagonist prevents neutrophil accumulation in hyperoxia-exposed newborn rats. J Pharmacol Exp Ther. 2001 Oct;299(1):90-5.

[2]. Milatovic S, et al. Impaired healing of nitrogen mustard wounds in CXCR2 null mice. Wound Repair Regen. 2003 May-Jun;11(3):213-9.

SB-265610物理化学性质

[ 密度 ]:
1.779 g/cm3

[ 沸点 ]:
527ºC at 760 mmHg

[ 分子式 ]:
C₁₄H₉BrN₆O

[ 分子量 ]:
357.16500

[ 闪点 ]:
272.5ºC

[ 精确质量 ]:
356.00200

[ PSA ]:
106.49000

[ LogP ]:
3.38208

[ 储存条件 ]:
2-8°C，密闭，干燥

SB-265610MSDS

详细MSDS(安全技术说明书)

SB-265610安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 危险品运输编码 ]:
NONH for all modes of transport

SB-265610文献

Regulation of CXCR2 expression and function by a disintegrin and metalloprotease-17 (ADAM17).

J. Leukoc. Biol. 97(3) , 447-54, (2015)

The chemokine receptor CXCR2 is expressed at high levels on circulating neutrophils and is critical for directing their migration to sites of inflammation. CXCR2 surface levels are rapidly modulated b...

Discovery of Novel CXCR2 Inhibitors Using Ligand-Based Pharmacophore Models.

J. Chem. Inf. Model. 55 , 1720-38, (2015)

The chemokine receptor CXCR2 is expressed on various immune cells and is essential for neutrophil recruitment and angiogenesis at sites of acute and chronic inflammation caused by tissue injury or inf...

Mesenchymal transition and dissemination of cancer cells is driven by myeloid-derived suppressor cells infiltrating the primary tumor.

PLoS Biol. 9 , e1001162, (2011)

In order to metastasize, cancer cells need to acquire a motile phenotype. Previously, development of this phenotype was thought to rely on the acquisition of selected, random mutations and thus would ...

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