PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC 50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
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Product Description
PTGR2-IN-1 is a potent PTGR2 inhibitor with an IC 50 of ~0.7 μM. PTGR2-IN-1 increases 15-keto-PGE2-dependent PPARγ transcriptional activity in PTGR2-transfected HEK293T cells.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Names and Identifiers
Smiles
COC1=CC=CC=C1N2CCN(CC2)C(=O)CC3=CC=CC=C3
Molecular Weight
310.4
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