MPO-0186 is microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor. MPO-0186 inhibited the production of PGE2 (IC50: 0.24 μM) in A549 cells via inhibition of mPGES-1 (IC50: 0.49 μM in a cell-free assay) and was found to be approximately 9- and 8-fold more potent than MK-886 as a reference inhibitor, respectively. A molecular docking study theoretically suggests that MPO-0186 could inhibit PGE2 production by blocking the PGH2 binding site of mPGES-1 enzyme. Furthermore, MPO-0186 demonstrated good liver metabolic stability and no significant inhibition observed in clinically relevant CYP isoforms except CYP2C19.
MedKoo Cat#: 464522
Name: MPO-0186
CAS#: unknown
Chemical Formula: C30H29ClN2O4S
Exact Mass: 548.1537
Molecular Weight: 549.08
Elemental Analysis: C, 65.62; H, 5.32; Cl, 6.46; N, 5.10; O, 11.66; S, 5.84
The following data is based on the product molecular weight 549.08 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
