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Danirixin

Danirixin (GSK1325756) 是一种选择性可逆的CXCR2拮抗剂，抑制 CXCL8 的IC50值为 12.5 nM。

CAS号

954126-98-8

分子式

C19H21ClFN3O4S

主要靶点

CXCR

仅限科研使用

Cat No : CM03605

Print datasheet

Synonyms

GSK1325756

验证数据展示

  • CAS No.: 954126-98-8

    Danirixin
    CAS#: 954126-98-8

产品信息

Danirixin is a potent antagonist of CXCR2 that inhibits IL-8 binding to CXCR2 (IC50: 12.5 nM).

CAS号 954126-98-8
分子式 C19H21ClFN3O4S
主要靶点 CXCR
主要通路 G蛋白偶联受体|自噬|免疫与炎症
分子量 441.9
纯度 99.78%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 GSK1325756

靶点活性

CXCL8-CXCR2:12.5 nM (cell free)

体内活性

Systemic exposure following single doses of danirixin 10 mg, 25 mg, 50 mg, 100 mg, and 200 mg increased with increasing dose. Engagement of pharmacology was demonstrated as inhibition of ex-vivo CXCL1-induced CD11b expression on peripheral blood neutrophils when compared to placebo (approximately 50 % for 50 mg and 100 mg danirixin, and 72 % at 200 mg). There was a 37 % decrease in Cmax and a 16 % decrease in AUC (0-∞) following administration of danirixin in the presence of food. Cmax also decreased by 65 % when danirixin 100 mg was administered following omeprazole 40 mg once daily for 5 days [1].

溶解度

DMSO:8 mg/mL (18.10 mM),Sonification/heating is recommended.

参考文献

1.Miller BE, et al. The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)--a selective CXCR2 antagonist --in healthy adult subjects. BMC Pharmacol Toxicol. 2015 Jun 20;16:18.
2.Miller BE, et al. The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers. Eur J Drug Metab Pharmacokinet. 2014 Sep;39(3):173-81.

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