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|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
TISSUE REGENERATION. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration.
Zhang Y,et.al. Science. 2015 Jun 12;348(6240). PMID: 26068857.
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