PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC 50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. In Vitro PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC 50 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 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PAT-505 suppresses ATX lysoPLD activity with an average IC 50 value of 62 nM and an average IC 90 value of 630 nM in mouse plasma, and the IC 90 in rat plasma is ∼770 nM. PAT-505 (30 mg/kg, p.o.) significantly reduces fibrotic score, the percentage of PSR-positive area, and α-SMA immunoreactivity in mouse model of nonalcoholic steatohepatitis (NASH) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:Autotaxin 2 nM (IC 50 , In Hep3B cells) Autotaxin 9.7 nM (IC 50 , In human blood ) Autotaxin 62 nM (IC 50 , In mouse plasma)
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PAT-505
CAS number：1782070-22-7 molecular formula：C23H18ClF2N3O2S
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| Chinese alias | - | ||
| English alias | 3-((6-chloro-2-cyclopropyl-1-(1-ethyl-1H-pyrazol-4-yl)-7-fluoro-1H-indol-3-yl)thio)-2-fluorobenzoic acid | 3-[6-chloro-2-cyclopropyl-1-(1-ethylpyrazol-4-yl)-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid | Benzoic acid, 3-((6-chloro-2-cyclopropyl-1-(1-e | ||
| CAS number | 1782070-22-7 | molecular formula | C23H18ClF2N3O2S |
| molecular weight | 473.92 g/mol | Exact mass | ≥98% |
| PSA | 85.400 Ų | logp | 5.300 |
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