PeptideDB

ATX inhibitor 5

CAS: 2402772-45-4 F: C22H18ClF3N6O W: 474.87

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows
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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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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.