Home Immunology & Inflammation CXCR antagonist - Interleukins inhibitor Danirixin (GSK1325756) For research use only.

Danirixin (GSK1325756)

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 (GSK1325756) Chemical Structure

Danirixin (GSK1325756) Chemical Structure

CAS No. 954126-98-8

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Danirixin (GSK1325756) Related Products

Signaling Pathway

CXCR Signaling Pathways

CXCR Signaling Pathway

Biological Activity

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.
Targets
CXCR2 [2] CXCL8 [2]
12.5 nM
In vitro
In vitro

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[1].
In Vivo
In vivo

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[1].
Animal Research Animal Models Male Lewis rats (275-400 g)
Dosages 25, 50, 150, or 500 mg/kg per day once daily
Administration by oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03457727 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 March 7 2018 Phase 1
NCT03136380 Completed
Pulmonary Disease Chronic Obstructive
GlaxoSmithKline
 May 10 2017 Phase 1

Chemical Information & Solubility

Molecular Weight 441.90 Formula

C19H21ClFN3O4S
CAS No. 954126-98-8 SDF --
Smiles CC1=C(C=CC=C1F)NC(=O)NC2=C(C(=C(C=C2)Cl)S(=O)(=O)C3CCCNC3)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 88 mg/mL ( (199.14 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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