SW033291 inhibition of 15-PGDH was noncompetitive versus PGE2 over concentrations up to 40 μM PGE2. SW033291 also demonstrated selective high-affinity interaction with 15-PGDH in thermal denaturation assays. Treatment of A549 cells with SW033291 increased PGE2 levels by 3.5-fold at 500 nM, with 50% of maximal stimulation (EC50) at ~75 nM.
 |
Source | Sci Rep (2018). Figure 5. SW033291 |
| Method | Treatment of diseased tendon stromal cells with inhibitors of 15-PGDH | |
| Cell Lines | tendon stromal cells | |
| Concentrations | 25 μM | |
| Incubation Time | 2 h | |
| Results | In incubations of IL-1β stimulated diseased tendon stromal cells with either indomethacin or SW033291, we found significantly lower concentrations of 15-oxo-LXA4 and 14-oxo-MaR1 levels, and a corresponding increase in the levels of 15-epi-LXA4 and MaR1 |
| Molecular Weight | 412.59 |
| Formula | C21H20N2OS3 |
| CAS Number | 459147-39-8 |
| Solubility (25°C) | DMSO 40 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.
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