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ATN-161 TFA salt is a novel small peptide inhibitor of integrin α5β1; a beta integrin antagonist with antitumor activity. ATN-161 TFA inhibited VEGF-induced migration and capillary tube formation in hCECs.
In vivo, injection of ATN-161 after laser photocoagulation inhibited CNV leakage and neovascularization to an extent similar to AF564. Furthermore, SD-OCT and histologic examinations indicated that ATN-161 significantly decreased the size of laser-induced lesions. Treatment with the α5β1 signaling inhibitor ATN-161 significantly blunts atherosclerotic plaque development in apolipoprotein E-deficient mice, characterized by reduced vascular cell adhesion molecule-1 expression and macrophage accumulation without affecting fibrous cap size.
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Source | Graefes Arch Clin Exp Ophthalmol (2018). Figure 2. ATN-161 |
| Method | western blot assay | |
| Cell Lines | Tet/opsin/VEGF mice | |
| Concentrations | 0.1, 1, and 10 μg/μL | |
| Incubation Time | 24 h | |
| Results | The analysis of western blot results revealed that ATN-161 significantly reduced the expression of integrin 5β1 at concentrations of 1 and 10 μg/μL, and this seemed to present a dose-independent manner |
| Molecular Weight | 711.67 |
| Formula | C25H36F3N9O10S |
| CAS Number | 904763-27-5 |
| Solubility (25°C) | Water 8 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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