货号	规格	价格	上海	北京	珠海	重庆	武汉
S87524-1mg买3赠1	99.50%	￥120.00 S87524-1mg ￥120.00 现货（买3赠1）	9 9	-	-	-	-
S87524-5mg买3赠1	99.50%	￥260.00 S87524-5mg ￥260.00 现货（买3赠1）	5 5	-	-	-	-
S87524-10mg买3赠1	99.50%	￥500.00 S87524-10mg ￥500.00 现货（买3赠1）	6 6	-	-	-	-
S87524-25mg	99.50%	￥860.00 S87524-25mg ￥860.00 现货	6 6	-	-	-	-
S87524-100mg	≥98%	￥2990.00 S87524-100mg ￥2990.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Danirixin (GSK1325756)是高亲和力的选择性CXCR2拮抗剂，抑制CXCL8 (IL-8)结合的IC50值为12.5 nM

靶点：

CXCR2; CXCL8:12.5 nM;CXCR

体外研究：

Danirixin has high affinity for CXCR2, with a negative log of the 50% inhibitory concentration (pIC50) of 7.9 for binding to Chinese hamster ovary cell (CHO)-expressed human CXCR2, and 78-fold selectivity over binding to CHO-expressed CXCR1. Danirixin is a competitive antagonist against CXCL8 in Ca2+-mobilization assays, with a KB of 6.5 nM and antagonist potency (pA2) of 8.44 and is fully reversible in washout experiments over 180 minutes

体内研究：

In rat and human whole-blood studies assessing neutrophil activation by surface CD11b expression following CXCL2 (rat) or CXCL1 (human) challenge, danirixin blocks the CD11b upregulation with pIC50s of 6.05 and 6.3, respectively. Danirixin dosed orally also blocks the influx of neutrophils into the lung in vivo in rats following aerosol lipopolysaccharide or ozone challenge, with median effective doses (ED50s) of 1.4 and 16 mg/kg respective

动物实验：

Animal Models: Male Lewis rats (275-400 g) Dosages: 25, 50, 150, or 500 mg/kg per day once daily Administration: by oral gavage

参考文献：

1. Busch-Petersen J, et al. Danirixin: A Reversible and Selective Antagonist of the CXC Chemokine Receptor 2. J Pharmacol Exp Ther. 2017, 362(2):338-346. 2. Bruce E. Miller, et al. The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756) − a selective CXCR2 antagonist − in healthy adult subjects. BMC Pharmacol Toxicol. 2015, 16: 18.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.263 ml	11.315 ml	22.629 ml
5 mM	0.453 ml	2.263 ml	4.526 ml
10 mM	0.226 ml	1.131 ml	2.263 ml
50 mM	0.045 ml	0.226 ml	0.453 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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