Danirixin

SKU: orb1302008

Description

Danirixin (GSK1325756) is a selective and potent CXCR2 antagonist, inhibiting IL-8 binding with an IC50 of 12.5 nM. This small molecule is a valuable research tool for investigating the role of CXCR2 in neutrophil-mediated inflammation in both in vitro and in vivo models.

Research Area

Cell Biology, Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 954126-98-8
• MW: 441.9
• Purity: 98.00% (May vary between batches)
• Formula: C₁₉H₂₁ClFN₃O₄S
• SMILES: Cc1c(F)cccc1NC(=O)Nc1ccc(Cl)c(c1O)S(=O)(=O)[C@H]1CCCNC1
• Target: CXCR
• Solubility: DMSO:60 mg/mL (135.78 mM);10% DMSO+40% PEG300+5% Tween-80+45% Saline:5 mg/mL (11.31 mM)

Bioactivity

• Target IC50:
  CXCL8-CXCR2:12.5 nM (cell free)
• In Vivo:
  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 .

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Danirixin, CXC chemokine receptors, CXCR, CXCR2, Inhibitor, GSK 1325756, GSK1325756, GSK-1325756, inhibit

Compound Identifiers

PubChem CID

24780598