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PTGR2-IN-1

Names

[ CAS No. ]:
349093-44-3

[ Name ]:
PTGR2-IN-1

[Synonym ]:
Ethanone, 1-[4-(2-methoxyphenyl)-1-piperazinyl]-2-phenyl-
1-[4-(2-Methoxyphenyl)-1-piperazinyl]-2-phenylethanone

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Others
Signaling Pathways >> Others >> Others

[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[1].

[References]

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

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
512.9±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C19H22N2O2

[ Molecular Weight ]:
310.390

[ Flash Point ]:
264.0±30.1 °C

[ Exact Mass ]:
310.168121

[ LogP ]:
2.65

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.588

[ Storage condition ]:
-20°C

Safety Information

[ Hazard Codes ]:
Xn

Related Compounds