Potent and selective vanin 1 inhibitor
PFI 653 is a potent and selective vanin 1 inhibitor (IC50 values in the range 6.85 - 24.5 nM). The compound exhibits selectivity over a panel of 40 kinases and a selection of 35 other targets including enzymes, receptors and ion channels (IC50 vs biotinidase >50 μM). Following administration of a single dose of PFI 653 (2 mg/kg iv) in rats AUC is 1790 ng.h/mL, half-life is 1 h and clearance is 19 mL/min/kg. Following oral administration of PFI 653 in solution, bioavailablility is 96%. In mice with DSS-induced inflammatory bowel disease (IBD), oral adminstration of PFI 653 dose-dependently reduces vanin 1 enzyme activity and disease symptoms.
| Marque | Tocris Bioscience |
|---|---|
| Réf. B-LABO | BL-RE-160809 |
| Réf. fabricant | 18744524 |
| Nom chimique ou matériau | 8-Oxa-2-azaspiro[4.5]dec-2-yl[2-[(2-pyrazinylmethyl)amino]-5-pyrimidinyl]methanone |
| CAS | 2173134-00-2 |
| Quantité | 50 mg |
| Cible | Vanin-1/VNN1 |
| Formule moléculaire | C<sub>18</sub>H<sub>22</sub>N<sub>6</sub>O<sub>2</sub> |
| Pureté | 0.98 |
