MF63MF63
MedChemExpress (MCE)
HY-13283
892549-43-8
99.55%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Room temperature in continental US
may vary elsewhere.
MF63 is a selective and orally active inhibitor of mPGES-1. MF63 reduces the accumulation of PGE2, relieves pyresis, hyperalgesia, and inflammatory pain by inhibiting mPGES-1.
MF63 (0.01-100 µM
24 h) selectively inhibits PGE2 induced by 10 ng/mL IL-1β in A549 cells, and increases the formation of PGF2α in a dose-dependent manner[1]. MF63 (10 µM
24 h) enhances the expression of various metallothionein 1 (MT1) subtypes and endogenous antagonists of IL-1 and IL-36 with the anti-inflammatory effects[2].
MF63 (100 mg/kg
p.o.
single dose) attenuates PEG2 accumulation in air pouches and brains of the KI (knock-in mPGES-1 gene) mice and inhibits PEG2 formation in a dose-dependent manner[1]. MF63 (10 mg/kg and 100 mg/kg
p.o.
single dose) inhibits the hyperalgesic response induced by LPS in the KI mice, with dose-dependently manner[1]. MF63 (0-150 mg/kg
p.o.
single dose) inhibits PEG2 synthesis, hyperalgesia, pyresis and relieves Chronic Osteoarthritic-Like Pain in the guinea pig[1]. MF63 (0-100 mg/kg
p.o.
twice daily for 4 days) has gastrointestinal tolerability in KI mice and nonhuman primates[1].
mPGES-1[1] Cellular Effect Cell Line Type Value Description References
| | | |
| | | | | |
[1]. Xu D, et al. MF63 [2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile], a selective microsomal prostaglandin E synthase-1 inhibitor, relieves pyresis and pain in preclinical models of inflammation. J Pharmacol Exp Ther. 2008 Sep
326(3):754-63. [Content Brief]
[2]. Tuure L, et al. Regulation of gene expression by MF63, a selective inhibitor of microsomal PGE synthase 1 (mPGES1) in human osteoarthritic chondrocytes. Br J Pharmacol. 2020 Sep
177(18):4134-4146.