PAT-505 是一种有效，选择性的，非竞争性的可口服的 autotaxin 抑制剂，在 Hep3B 中，抑制 autotaxin 的活性，IC₅₀ 值为 2 nM，在人血液和小鼠血浆中，IC₅₀ 值分别为 9.7 nM 和 62 nM。

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.

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Autotaxin 2 nM (IC50, In Hep3B cells) Autotaxin

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 μM. has not independently confirmed the accuracy of these methods. They are for reference only.

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). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Bain G, et al. Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis. J Pharmacol Exp Ther. 2017 Jan;360(1):1-13. Epub 2016 Oct 17.

In Vitro: DMSO : 48.33 mg/mL (101.98 mM; Need ultrasonic)配制储备液