Ladarixin sodium

CAS No. 865625-56-5

Ladarixin sodium( DF-2156 | DF-2156A )

Catalog No. M16289 CAS No. 865625-56-5

A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Ladarixin sodium
  • Note
    Research use only, not for human use.
  • Brief Description
    A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM.
  • Description
    A novel allosteric, noncompetitive dual CXCR1/2 inhibitor that inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 in vitro with IC50 of 0.7 nM; prevents PMN infiltration and tissue damage in several models of IR injury in vivo; abrogates motility and induces apoptosis in cultured cutaneous and uveal melanoma cells and xenografts; also prevents inflammation-mediated damage in MLD-STZ, prevents and reverses diabetes in NOD mice.Diabetes Phase 2 Clinical.
  • In Vitro
    Ladarixin inhibits human polymorphonuclear leukocyte (PMN) migration to CXCL8 (IC50 at 0.7 nM).
  • In Vivo
    Ladarixin (10 mg/kg; p.o. once a day) reduces allergic airway inflammation in a model of single OVA exposure. Ladarixin reduces allergic airway inflammation, remodeling, and bronchial hyperreactivity in a model of chronic OVA exposure.Ladarixin (10 mg/kg; p.o. once a day for 8 days) reduces pulmonary inflammation and fibrosis induced by bleomycin in mice.Ladarixin (10 mg/kg; p.o. once a day for 3 days) protects mice from cigarette smoke-induced exacerbation of influenza-A infection.Ladarixin is also effective in decreasing CXCL8-induced polymorphonuclear leukocyte infiltration in several animal models without a significant dose-related reduction in systemic neutrophil counts. Animal Model:Mice (cigarette smoke-induced exacerbation of Influenza-A infection model)Dosage:10 mg/kg Administration:P.o. once a day at days 2, 3 and 4 post-infection Result:Significantly attenuated the exacerbation in lethality and respiratory changes noted in CSFlu group.
  • Synonyms
    DF-2156 | DF-2156A
  • Pathway
    GPCR/G Protein
  • Target
    Chemokine Receptor
  • Recptor
    Chemokine Receptor
  • Research Area
    Metabolic Disease
  • Indication
    Diabetes

Chemical Information

  • CAS Number
    865625-56-5
  • Formula Weight
    397.315
  • Molecular Formula
    C11H11F3NNaO6S2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (251.69 mM)
  • SMILES
    CC(C1=CC=C(C=C1)OS(=O)(=O)C(F)(F)F)C(=O)[N-]S(=O)(=O)C.[Na+]
  • Chemical Name
    4-((2R)-1-Oxo-1-(methanesulfonamido)propan-2-yl)phenyl trifluoromethanesulfonate sodium salt

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Garau A, et al. Eur Cytokine Netw. 2006 Mar;17(1):35-41. 2. Citro A, et al. Diabetes. 2015 Apr;64(4):1329-40. 3. Kemp DM, et al. Oncotarget. 2017 Feb 28;8(9):14428-14442. 4. Bertini R, et al. Br J Pharmacol. 2012 Jan;165(2):436-54.
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