Danirixin (GSK1325756)

For research use only. Not for use in humans.

Catalog No.S6620

1 publication

Danirixin (GSK1325756) Chemical Structure

Molecular Weight(MW): 441.90

Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.

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Selleck's Danirixin (GSK1325756) has been cited by 1 publication

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Biological Activity

Description Danirixin (GSK1325756) is a small molecule, non-peptide, high affinity (IC50 for CXCL8 binding = 12.5 nM), selective, and reversible CXCR2 antagonist.
Targets
CXCL8 [2]
()
12.5 nM
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 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].

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: Male Lewis rats (275-400 g)
  • Formulation: 20% PEG and 16% (40% w/v, hydroxylpropyl β-cyclodextrin, pH 4.0
  • Dosages: 25, 50, 150, or 500 mg/kg per day once daily
  • Administration: by oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (199.14 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 441.90
Formula

C19H21ClFN3O4S

CAS No. 954126-98-8
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C(NC(=O)NC2=C(O)C(=C(Cl)C=C2)[S](=O)(=O)C3CCCNC3)C=CC=C1F

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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.

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CXCR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID