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 |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related Integrin Products |
|---|
| HSDVHK-NH2
HSDVHK-NH2 is an antagonist of the integrin αvβ3-vitronectin interaction, with an IC50 of 1.74 pg/mL (2.414 pM). |
| LDV
LDV, a tripeptide, is a non-fluorescent analog of LDV-FITC. |
| Cyclo(RADfK)
Cyclo(RADfK) is a selective α(v)β(3) integrin ligand that has been extensively used for research, therapy, and diagnosis of neoangiogenesis. |
| Obtustatin
Obtustatin is a non-RGD disintegrin of 41 residues. |
| Integrin Binding Peptide
Integrin Binding Peptide is derived by fibronectin. |
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