T0070907 is a potent and selective PPARγ inhibitor with IC50 of 1 nM, with a >800-fold selectivity over PPARα and PPARδ.
 |
Source | Environ Health Perspect (2018). Figure 3. T0070907 |
| Method | Adipogenic Differentiation | |
| Cell Lines | human and mouse MSCs | |
| Concentrations | 100nM | |
| Incubation Time | 8h | |
| Results | In hMSCs, T0070907 (100nM) significantly blocked the ability of DBT to induce the accumulation of lipids |
| Cell Experiment | |
|---|---|
| Cell lines | Vascular endothelial cells (VECs) |
| Preparation method | Cellular impedance assay VEC proliferation was assessed using a cellular impedance assay. VECs were seeded into 8-well E-plates (ACEA Biosciences, Inc., San Diego, CA, USA) at a density of 7,500 cells/well and cultured overnight. Cells were cultured with complete medium, supplemented with 0.1% dimethyl sulfoxide (DMSO) as a control, the PPARγ agonist rosiglitazone (10 µM) or the PPARγ antagonist T0070907 (15 µM) respectively, as previously described. Cellular proliferation was dynamically monitored using the iCELLigence™ real-time cell analysis (RTCA) system (ACEA Biosciences, Inc.) at 37°C in a 5% CO2 atmosphere for 100 h. The cell index, which reflects the adhesion, proliferation and viability of the cells through electrical impedance across interdigitated microelectrodes integrated on the bottom of the E-plates, was automatically calculated for each E-plate well using RTCA software version 1.2 (Roche Diagnostics, Basel, Switzerland) and graphs were generated in real-time using the iCELLigence™ system (30,31). Each treatment was performed in duplicate and three independent experiments were conducted. |
| Concentrations | 15 µM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Preconditioning is performed by administering a low dose (1 mg/kg) of Escherichia coli LPS (serotype 0.127:B8) intraperitoneally 24 hr before the induction of severe endotoxemia |
| Formulation | 10% v/v dimethylsulfoxide [DMSO], 20–25% v/v DMSO, or saline |
| Dosages | 1 mg/kg |
| Administration | intraperitoneally |
| Molecular Weight | 277.66 |
| Formula | C12H8ClN3O3 |
| CAS Number | 313516-66-4 |
| Solubility (25°C) | DMSO 30 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.
[4] Zhengzhe An, et al. T0070907 inhibits repair of radiation-induced DNA damage by targeting RAD51
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