SX-517

Names

[ Name ]:
SX-517

[Synonym ]:
Boronic acid, B-[2-[[[5-[[(4-fluorophenyl)amino]carbonyl]-2-pyridinyl]thio]methyl]phenyl]-
{2-[({5-[(4-Fluorophenyl)carbamoyl]-2-pyridinyl}sulfanyl)methyl]phenyl}boronic acid
SX-517

Biological Activity

[Description]:

A potent, specific, noncompetitive dual CXCR1 and CXCR2 antagonist with IC50 of 38 nM (vs. CXCL1) and 36 nM (vs. CXCL8), respectively; inhibits CXCL1-induced Ca(2+) flux in human PMNs but has no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF; antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation in recombinant HEK293 cells expressed CXCR2; significantly inhibits inflammation in an in vivo murine model (0.2 mg/kg iv).

[References]

References 1. Maeda DY, et al. J Med Chem. 2014 Oct 23;57(20):8378-97. 2. Schuler AD, et al.Bioorg Med Chem Lett. 2015 Sep 15;25(18):3793-7. View Related Products by Target Chemokine Receptor (CCR and CXCR)

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₁₉H₁₆BFN₂O₃S

[ Molecular Weight ]:
382.216

[ Exact Mass ]:
382.095886

[ LogP ]:
3.98

[ Index of Refraction ]:
1.663

Related Compounds

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