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mPGES1-IN-17d

Chemical Structure mPGES1-IN-17d

CAS No.: 1469976-70-2

mPGES1-IN-17d

Catalog No.: PC-62797Not For Human Use, Lab Use Only.

mPGES1-IN-17d is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM, human whole blood IC50 of 249.9 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

mPGES1-IN-17d is a potent, selective mPGES-1 inhibitor with enzyme IC50 of 8 nM, A549 cell IC50 of 16.24 nM, human whole blood IC50 of 249.9 nM; displays excellent in vitro selectivity over mPGES-2, cPGES, COX1/2, other prostanoid synthases, favorable hERG and CEREP panel profile; shows good efficacy in LPS-induced thermal hyperalgesia pain model; demonstrates good oral pharmacokinetic profiles and good CNS B/P ratio in rat and guinea pig.

Physicochemical Properties

M.Wt 538.859
Formula C24H16ClF5N4O3
CAS No. 1469976-70-2
Storage
Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 3 Month
Shipping
Solubility

Chemical Name

2-((2-chloro-6-fluorophenyl)amino)-N-(3-fluoro-5-(trifluoromethyl)phenyl)-1-methyl-7,8-dihydro-1H-[1,4]dioxino[2',3':3,4]benzo[1,2-d]imidazole-5-carboxamide

Clinical Information

References

1. Muthukaman N, et al. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5977-5984.

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