PTGR2-IN-1是一种有效的PTGR2抑制剂，IC50为~0.7μM。PTGR2-IN-1增加了转染PTGR2的HEK293T细胞15-keto-PGE2依赖的PPARγ转录活性。
货号:ajcx31902
CAS:349093-44-3
分子式:C19H22N2O2
分子量：310.39
溶解度:DMSO: 100 mg/mL (322.18 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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