PAT-505 B

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma.

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.

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 α-SMA immunoreactivity in mouse model of nonalcoholic steatohepatitis (NASH).

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Angiogenesis

EGFR

EGFR

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1782070-22-7

473.92

C23H18ClF2N3O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 48.33 mg/mL (101.98 mM; 超声助溶 )

CCn1cc(cn1)-n1c(C2CC2)c(Sc2cccc(C(O)=O)c2F)c2ccc(Cl)c(F)c12

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(-20℃)

With Ice Pack

≥ 2 years