For research use only.
CAS No. 954126-98-8
Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.
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|Description||Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 (IL-8) binding = 12.5 nM), selective, and reversible CXCR2 antagonist.|
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.
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 respectively.
|In vitro||DMSO||88 mg/mL (199.14 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03457727||Completed||Drug: Danirixin|Drug: Omeprazole||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||March 7 2018||Phase 1|
|NCT03136380||Completed||Drug: GSK1325756H|Drug: Placebo||Pulmonary Disease Chronic Obstructive||GlaxoSmithKline||May 10 2017||Phase 1|
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