For research use only. Not for therapeutic Use.
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[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].
| Catalog Number | I005345 |
| CAS Number | 892549-43-8 |
| Synonyms | 2-(6-chloro-3H-phenanthro[9,10-d]imidazol-2-yl)benzene-1,3-dicarbonitrile |
| Molecular Formula | C23H11ClN4 |
| Purity | ≥95% |
| InChI | InChI=1S/C23H11ClN4/c24-15-8-9-18-19(10-15)16-6-1-2-7-17(16)21-22(18)28-23(27-21)20-13(11-25)4-3-5-14(20)12-26/h1-10H,(H,27,28) |
| InChIKey | BVFLHOOKHPFDCT-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C(=C1)C3=C(C=CC(=C3)Cl)C4=C2N=C(N4)C5=C(C=CC=C5C#N)C#N |
| Reference | [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. [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. |
