VZRIHFZJVIOJBE-UHFFFAOYSA-N
- CAS No.
- 1240494-13-6
- Chemical Name:
- VZRIHFZJVIOJBE-UHFFFAOYSA-N
- Synonyms
- VZRIHFZJVIOJBE-UHFFFAOYSA-N;Boronic acid, B-[2-[[[5-[[(4-fluorophenyl)amino]carbonyl]-2-pyridinyl]thio]methyl]phenyl]-
- CBNumber:
- CB43396221
- Molecular Formula:
- C19H16BFN2O3S
- Molecular Weight:
- 382.22
- MDL Number:
- MFCD28963933
- MOL File:
- 1240494-13-6.mol
| Density | 1.39±0.1 g/cm3(Predicted) |
|---|---|
| pka | 8.45±0.53(Predicted) |
| form | Solid |
| color | White to off-white |
| FDA UNII | 36UH926WTQ |
VZRIHFZJVIOJBE-UHFFFAOYSA-N Chemical Properties,Uses,Production
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
VZRIHFZJVIOJBE-UHFFFAOYSA-N Preparation Products And Raw materials
VZRIHFZJVIOJBE-UHFFFAOYSA-N Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6312 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; | support@targetmol.com | United States | 39035 | 58 |
| Tianjin Kailiqi Biotechnology Co., Ltd. | 15076683720 | klq@cw-bio.com | China | 8011 | 55 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29257 | 58 |
