ATX inhibitor 18

Names

[ Name ]:
ATX inhibitor 18

Biological Activity

[Description]:

ATX inhibitor 18 is a potent ATX inhibitor with an IC50 value of 24.2 nM. ATX inhibitor 18 shows antiproliferative activity and anti-fibrosis activity. ATX inhibitor 18 suppresses collagen deposition in TGF-β-mediated cardiac fibrosis[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

[Target]

Autotaxin:24.2 nM (IC50)

[In Vitro]

ATX inhibitor 18 (compound 8b) (10 µM; 48 h) 在 CFs、t-HSC/Cl-6 细胞中显示出抗增殖活性[1]。 TX inhibitor 18 (0-4 µM) 具有抗纤维化活性，对 CF、t-HSC/Cl-6 细胞的 IC50 值分别为 0.87 和 1.10 µM[1]。 Cell Viability Assaysup>[1] Cell Line: CFs, t-HSC/Cl-6 cells Concentration: 10 µM Incubation Time: 48 h Result: Showed antiproliferative activity with inhibitory activity of 81.5% and 79.4% for CFs, t-HSC/Cl-6 cells, respectively.

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₁H₁₇Cl₂FN₆O

[ Molecular Weight ]:
459.30

Related Compounds

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