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PAI-039 exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to clinical trials. PAI-039 exerts antithrombotic efficacy in rat models of arterial and venous vascular injury without effecting platelet aggregation. A first study demonstrates dose related effects of PAI-039 on increasing thrombus resolution and inferior vena cava blood flow without adverse effects on anti-coagulation in a rat stenosis model of venous thrombosis.
| Cell Experiment | |
|---|---|
| Cell lines | T24, UM-UC-14, UROtsa, and HeLa cells |
| Preparation method | Briefly,plating cell lines, T24, UM-UC-14, UROtsa, and HeLa cells in 96-well dishes in triplicate at 1 ×103 cells per well and allowing to adhere for 24 hours. Subsequently, adding tiplaxtinin to the wells and allowing to incubate at the indicated concentrations.Determining cellular proliferation by CellTiter-Glo Luminescent Cell Viability Assay according to manufacturer's instructions at 24 hours, and determining IC50 of tiplaxtinin in Graphpad Prism. Using a FLUOstar OPTIMA Reader to measure Luminescence . |
| Concentrations | ~50 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Rat with carotid thrombosis |
| Formulation | 2.0% Tween 80/0.5% methylcellulose |
| Dosages | 1 mg/kg |
| Administration | p.o. |
| Molecular Weight | 439.38 |
| Formula | C24H16F3NO4 |
| CAS Number | 393105-53-8 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[4] Lijnen HR, et al. Thromb Haemost. Tiplaxtinin impairs nutritionally induced obesity in mice.
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