ATX inhibitor 5

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

ATX inhibitor 5 是有效的口服活性 autotaxin (ATX) 抑制剂，IC50 为 15.3 nM。AATX inhibitor 5 具有抗肝纤维化作用，并显着降低 CCl4 诱导的肝纤维化水平。

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.

ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC).ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β.Cell Proliferation Assay Cell Line:CFs and t-HSC/Cl-6 cells Concentration:0.0001, 0.01, 1, 100, 10000 μM Incubation Time:48 hours Result:Displayed activities against CFs and t-HSC/Cl-6 cells with IC50s of 1.21 and 0.78 μM, respectively.

ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently.Animal Model:Male Konmin mice (8-week old, 22-25 g)Dosage:20, 40 mg/kg Administration:Orally; once daily for two weeks Result:Prominently reduced CCl4-induced hepatic fibrosis level.

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Angiogenesis

PDE

PDE

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2402772-45-4

474.87

C22H18ClF3N6O

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (526.46 mM; 超声助溶 )

FC(F)(F)c1cccc(Nc2ncnc3CCN(Cc23)C(=O)N\N=C\c2ccc(Cl)cc2)c1

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(-20℃)

With Ice Pack

≥ 2 years