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PXS 4728A
- PXS 4728 HCl - BI-1467335
- Parent CAS: 1478364-40-7
- Soluble in water and DMSO
- MF: C15H21FN2O2.HCl
- MW: 316.8
Description
PXS 4728A (BI-1467335) is a highly potent and orally available inhibitor of VAP-1/SSAO, (encoded by the AOC3 gene) with an IC50 value 5 nM and greater than 500-fold selectivity against related human amine oxidases. By inhibiting SSAO enzymatic activity, it impairs neutrophil tethering and rolling along the vascular endothelium, keeping white blood cells from entering tissues. It stops SSAO from breaking down primary amines, which cuts off the production of harmful byproducts like hydrogen peroxide and reactive aldehydes.
VAP-1/SSAO pharmacology is highly relevant to COPD, NASH, and chronic inflammatory research; PXS-4728A serves as a potent chemical probe that supports mechanistic studies of VAP-1/SSAO inflammatory pathways across biochemical, cellular, and disease-model assays.
Key Features
- • VAP-1/SSAO inhibitor with IC50 of 5 nM
- • >500-fold selective over all the related human amine oxidases
- Modulates VAP-1-dependent biological activity
Applications
- VAP-1 pharmacology and target-validation studies
- VAP-1 inflammatory pathway studies
- Disease-model research related to COPD, NASH
- Compound profiling, assay development and lead-optimization support
More Information
| Parent CAS No. | 1478364-40-7 |
|---|---|
| Chemical Name | (E)-4-(2-(aminomethyl)-3-fluoroallyloxy)-N-tert-butylbenzamide hydrochloride |
| extra_info | Old price 25 mg @ €435 |
| SMILES | C(NC(C)(C)C)(=O)C1=CC=C(OC/C(/CN)=C/F)C=C1.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C15H21FN2O2.ClH/c1-15(2,3)18-14(19)12-4-6-13(7-5-12)20-10-11(8-16)9-17;/h4-8H,9-10,17H2,1-3H3,(H,18,19);1H/b11-8+; |
| InChiKey | AEMZEDNMNLIDSL-YGCVIUNWSA-N |
| CID | 71812246 |
| Short Description | VAP-1 inhibitor |
References
- M Wong et al. Semicarbazide-sensitive amine oxidase (SSAO) inhibition ameliorates kidney fibrosis in a unilateral ureteral obstruction murine model. Am J Physiol Renal Physiol. 2014 Oct 15;307(8):F908-16.
- HC Schilter et al. Effects of an anti-inflammatory VAP-1/SSAO inhibitor, PXS-4728A, on pulmonary neutrophil migration. Respir Res. 2015 Mar 20;16:42.
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