GSK1325756

• CAT Number: I005656
• CAS Number: 954126-98-8
• Molecular Formula: C₁₉H₂₁ClFN₃O₄S
• Molecular Weight: 441.9
• Purity: ≥95%
• Synonyms: GSK1325756;GSK1325756B
• Target: CXCL8
• Solubility: DMSO: ≤ 8 mg/mL
• Storage: -20°C
• IC50: 12.5 nM
• InChI: InChI=1S/C19H21ClFN3O4S/c1-11-14(21)5-2-6-15(11)23-19(26)24-16-8-7-13(20)18(17(16)25)29(27,28)12-4-3-9-22-10-12/h2,5-8,12,22,25H,3-4,9-10H2,1H3,(H2,23,24,26)/t12-/m0/s1
• InChIKey: NGYNBSHYFOFVLS-LBPRGKRZSA-N
• SMILES: CC1=C(C=CC=C1F)NC(=O)NC2=C(C(=C(C=C2)Cl)S(=O)(=O)C3CCCNC3)O

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


Danirixin is a small molecule CXCR2 antagonist being evaluated as a potential anti-inflammatory medicine. Danirixin has demonstrated potent antagonism of CXCR2 activity in vitro and anti-inflammatory effects in various preclinical models. Its pharmacologic activity and duration of action following oral administration support its potential use as an oral, anti-inflammatory agent. [1] Danirixin (GSK1325756) is a small, high-affinity, selective and reversible CXCR2 antagonist in development for treatment of chronic obstructive pulmonary disease. Danirixin (GSK1325756) is a small, non-peptide, high-affinity (IC50 for CXCL8 binding 12.5 nM), selective and reversible CXCR2 antagonist. Danirixin has demonstrated potent antagonism of CXCR2 activity, both in vitro and in vivo in preclinical studies. Its oral potency and duration of action support its potential use as an oral, anti-inflammatory agent in the treatment of disorders associated with the accumulation of neutrophils. [2]

Reference

1:Identification and characterisation of a salt form of Danirixin with reduced pharmacokinetic variability in patient populations. Bloomer JC, Ambery C, Miller BE, Connolly P, Garden H, Henley N, Hodnett N, Keel S, Kreindler JL, Lloyd RS, Matthews W, Yonchuk J, Lazaar AL.Eur J Pharm Biopharm. 2017 Apr 3. pii: S0939-6411(16)31009-8. doi: 10.1016/j.ejpb.2017.03.023. [Epub ahead of print] PMID: 28385615 2:The pharmacokinetics and pharmacodynamics of danirixin (GSK1325756)–a selective CXCR2 antagonist –in healthy adult subjects. Miller BE, Mistry S, Smart K, Connolly P, Carpenter DC, Cooray H, Bloomer JC, Tal-Singer R, Lazaar AL.BMC Pharmacol Toxicol. 2015 Jun 20;16:18. doi: 10.1186/s40360-015-0017-x. PMID: 26092545 Free PMC Article3:The pharmacokinetics of conventional and bioenhanced tablet formulations of danirixin (GSK1325756) following oral administration in healthy, elderly, human volunteers. Miller BE, Smart K, Mistry S, Ambery CL, Bloomer JC, Connolly P, Sanderson D, Shreeves T, Smith R, Lazaar AL.Eur J Drug Metab Pharmacokinet. 2014 Sep;39(3):173-81. doi: 10.1007/s13318-014-0179-8. Epub 2014 Feb 7. PMID: 24504700 Free PMC Article