| Identification | Back Directory | [Name]
VZRIHFZJVIOJBE-UHFFFAOYSA-N | [CAS]
1240494-13-6 | [Synonyms]
VZRIHFZJVIOJBE-UHFFFAOYSA-N | [Molecular Formula]
C19H16BFN2O3S | [MDL Number]
MFCD28963933 | [MOL File]
1240494-13-6.mol | [Molecular Weight]
382.22 |
| Hazard Information | Back Directory | [Description]
SX-517 is a potent noncompetitive boronic acid CXCR1/2 antagonist. SX-517 inhibited CXCL1-induced Ca(2+) flux (IC50 = 38 nM) in human PMNs but had no effect on the Ca(2+) flux induced by C5a, fMLF, or PAF. SX-517 is the first reported boronic acid chemokine antagonist and represents a novel pharmacophore for CXCR1/2 antagonism. | [Uses]
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model[1][2]. | [in vivo]
SX-517 (compound 7) (0.2 mg/kg; iv; single dose) significantly inhibits inflammation in an in vivo murine model[1].
| Animal Model: | Male CD1 SWISS mice with an air-pouch on the backs (10-15 week old)[1] | | Dosage: | 0.02 mg/kg, 0.2 mg/kg | | Administration: | Intravenous injection; single dose | | Result: | Significant reduction in cell count in the pouches of treated animals compared to the positive control cohort. |
| [IC 50]
CXCR2; CXCR1 | [References]
[1] 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2. J Med Chem. 2014 Oct 23;57(20):8378-97. DOI:10.1021/jm500827t
[2] Ti H, et al. Targeted Treatments for Chronic Obstructive Pulmonary Disease (COPD) Using Low-Molecular-Weight Drugs (LMWDs). J Med Chem. 2019 Jul 11;62(13):5944-5978. DOI:10.1021/acs.jmedchem.8b01520 |
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