Table 2 Selectivity profile of SNT-8370 against related amine oxidase and heme peroxidase targets

From: Targeting vascular adhesion protein-1 and myeloperoxidase with a dual inhibitor SNT-8370 in preclinical models of inflammatory disease

Amine Oxidase assaya,b

IC50 (μM)

Peroxidase assaya,b

IC50 (μM)

VAP-1, human

0.010

MPO, human

0.017

VAP-1, rat

0.005

MPO, mousec

0.10

VAP-1, dog

0.002

  

DAO, human

>30

TPO, humand

13

MAO-A, human

>30

LPO, bovine

7.5

MAO-B, human

13

EPO, human

11

LOX, human

>30

PXDN, human

7.9

  1. aThe measurement of enzymatic activities was based on the rate of production (amine oxidase) or consumption (peroxidase) of H2O2 using an Amplex Red assay or H2O2-specific microelectrode.
  2. bMinimum of n = 2 for each experiment.
  3. cMouse MPO activity was measured using the MAPS bioluminescence assay.
  4. dTPO activity was measured as the rate of ascorbic acid oxidation.