PTGR2-IN-1

• CAT Number: I045514
• CAS Number: 349093-44-3
• Molecular Formula: C19H22N2O2
• Molecular Weight: 310.39
• Purity: ≥95%
• Synonyms: 1-[4-(2-methoxyphenyl)piperazin-1-yl]-2-phenylethanone
• InChI: InChI=1S/C19H22N2O2/c1-23-18-10-6-5-9-17(18)20-11-13-21(14-12-20)19(22)15-16-7-3-2-4-8-16/h2-10H,11-15H2,1H3
• InChIKey: TVIOYMPBWXQRRQ-UHFFFAOYSA-N
• SMILES: COC1=CC=CC=C1N2CCN(CC2)C(=O)CC3=CC=CC=C3

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].
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].

Reference

[1]. Parker CG, et al. Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017;168(3):527-541.e29.
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