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PXS 4728A
- PXS 4728 HCl
- Parent CAS: 1478364-40-7
- Soluble in water and DMSO
- MF: C15H21FN2O2.HCl
- MW: 316.8
Description
Potent and orally available inhibitor of VAP-1 (aka SSAO/AOC3; IC50 value 5 nM), inhibiting neutrophil rolling and tethering in the mouse cremaster model, and showing >500-fold selectivity for VAP-1/SSAO over all the related human amine oxidases. PXS 4728 diminishes lung inflammation in a variety of models indicating proof of concept for a novel therapeutic approach in respiratory diseases that are characterized by neutrophilic pattern of inflammation. PXS 4728 is in clinical trials for the treatment of cardiometabolic diseases like the liver-related disease Nonalcoholic Steatohepatitis (NASH).
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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