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

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

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].

954126-98-8

C19H21ClFN3O4S

441.9

GSK1325756

DMSO:8 mg/mL (18.10 mM)),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years