| Bioactivity | 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[1]. | ||||||||||||
| Invitro | ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC)[1].ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
| In Vivo | ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently[1]. Animal Model: | ||||||||||||
| Name | ATX inhibitor 5 | ||||||||||||
| CAS | 2402772-45-4 | ||||||||||||
| Formula | C22H18ClF3N6O | ||||||||||||
| Molar Mass | 474.87 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Jiang N, et al.Optimization and evaluation of novel tetrahydropyrido[4,3-d]pyrimidine derivatives as ATX inhibitors for cardiac and hepatic fibrosis.Eur J Med Chem. 2020 Feb 1;187:111904. |