LY3023703 

LY3023703 is an orally active microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor. LY3023703 inhibits the production of PGE₂. LY3023703 is applicable to research related to inflammatory diseases and osteoarthritis pain^[1][2].

LY3023703 (Compound 8) potently inhibits human mPGES-1 microsomes, with an IC₅₀ of 0.9 nM^[1].
LY3023703 weakly inhibits rat mPGES-1 microsomes, with an IC₅₀ value of 33.9 μM^[1].
LY3023703 inhibits the production of PGE₂ in IL-1β-stimulated A549 cells with an IC₅₀ of 12 nM, without affecting the production of PGI₂^[1].
LY3023703 inhibits LPS (HY-D1056)-stimulated PGE₂ production in human whole blood, with an IC₅₀ of 12 nM and an IC₈₀ of 69 nM, without affecting the production of TXB₂ or PGF₂α^[1].
LY3023703 inhibits LPS-stimulated PGE₂ production in canine whole blood, with an IC₅₀ of 139 nM and an IC₈₀ of 703 nM^[1].
LY3023703 (10 μM; 30 min preincubation, 1 min reaction) weakly inhibits microsomal CYP3A4 in a time-dependent manner^[1].
LY3023703 inhibits hERG channels with an IC₅₀ of 82.6 μM, compared with an IC₈₀ of 69 nM against HWB PGE₂^[1].
LY3023703 (Compound 2) potently inhibits mPGES-1-mediated PGE₂ production in human whole blood, with an IC₅₀ of 0.012 μM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

495.45

C₂₃H₂₂F₅N₅O₂

1415089-24-5

O=C(C1=CC(CNC(C(C)C)=O)=CN=C1C(F)F)NC2=NC(C)=C(C3=CC=C(C(F)(F)F)C=C3)N2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Schiffler MA, et al. Discovery and Characterization of 2-Acylaminoimidazole Microsomal Prostaglandin E Synthase-1 Inhibitors. J Med Chem. 2016;59(1):194-205.  [Content Brief]

  [2]. Norman BH, et al. Identification and Mitigation of Reactive Metabolites of 2-Aminoimidazole-Containing Microsomal Prostaglandin E Synthase-1 Inhibitors Terminated Due to Clinical Drug-Induced Liver Injury. J Med Chem. 2018;61(5):2041-2051.