PAT-505

1782070-22-7

C23H18ClF2N3O2S

DMSO : 48.33 mg/mL (101.98 mM; Need ultrasonic)

Metabolic Enzyme/Protease

PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC₅₀ of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. IC50 & Target: IC50: 2 nM (Autotaxin, Hep3B cell), 9.7 nM (Autotaxin, Human blood), 62 nM (Autotaxin, Mouse plasma)^[1] In Vitro: PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC₅₀ of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. PAT-505 is selective for ATX versus other ENPP proteins, and shows marginal inhibition of radiolabeled agonist or antagonist binding to the adenosine A3 receptor, MT1 melatonin receptor, prostaglandin E2 EP4 receptor, 5-HT5a serotonin receptor, and GABA-gated Cl^- channel with 50%-70% inhibition at 10 uM^[1]. In Vivo: PAT-505 suppresses ATX lysoPLD activity with an average IC₅₀ value of 62 nM and an average IC₉₀ value of 630 nM in mouse plasma, and the IC₉₀ in rat plasma is ?770 nM. PAT-505 (30 mg/kg, p.o.) significantly reduces fibrotic score, the percentage of PSR-positive area, and alpha-SMA immunoreactivity in mouse model of nonalcoholic steatohepatitis (NASH)^[1].