1240494-13-6

1240494-13-6 structure

Name: SX-517
Chemical Name: SX-517
CAS Number: 1240494-13-6
Molecular Formula: C₁₉H₁₆BFN₂O₃S
Molecular Weight: 382.216
Catalog: Signaling Pathways GPCR/G Protein CXCR
Create Date: 2020-01-11 19:17:50
Modify Date: 2024-02-28 18:33:55
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).

Name	SX-517
Synonyms	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

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)