| Bioactivity | PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells[1]. | |||||||||
| Invitro | A screen of structural analogs of 20 identified PTGR2-IN-1, which shows substantially increased potency (>20-fold) in assays measuring either competition of 8-labeling or 15-keto-PGE2 reductase activity (IC50 = 0.6 μM) of recombinant PTGR2, as well as an inactive control compound 23. PTGR2-IN-1 (Compound 22) blocks FFF 8 labeling of endogenous PTGR2 in HEK293T cells with good potency (complete inhibition at 5 μM and ~80% inhibition at 500 nM) and excellent selectivity[1]. | |||||||||
| Name | PTGR2-IN-1 | |||||||||
| CAS | 349093-44-3 | |||||||||
| Formula | C19H22N2O2 | |||||||||
| Molar Mass | 310.39 | |||||||||
| Appearance | Oil | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. Parker CG, et al. Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017;168(3):527-541.e29. |