MF63 | CAS:892549-43-8

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Name:MF63; 
Cat. No. :CS-0508
CAS No. :892549-43-8
Formula:C23H11ClN4
M. Wt. : 378.81
Solubility:DMSO: ≥ 43 mg/mL

MF63 is a selective mPGES-1 inhibitor with an IC50 of 0.9 nM and 1.3 nM for pig mPGES-1 and human mPGES-1 enzyme, respectively. IC50 value: 0.9 nM ( pig mPGES-1); 1.3 nM (human mPGES-1)Target: mPGES-1MF63 potently inhibited the human mPGES-1 enzyme with a high degree (>1000-fold) of selectivity over other prostanoid synthases. In rodent species, MF63 strongly inhibited guinea pig mPGES-1 but not the mouse or rat enzyme. When tested in the guinea pig and a knock-in (KI) mouse expressing human mPGES-1, the compound selectively suppressed the synthesis of PGE(2), but not other prostaglandins inhibitable by nonsteroidal anti-inflammatory drugs (NSAIDs), yet retained NSAID-like efficacy at inhibiting lipopolysaccharide-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.

Baragatti B, Coceani F.,Dual, constrictor-to-dilator, response of the mouse ductus arteriosus to the microsomal prostaglandin E synthase-1 inhibitor, 2-(6-chloro-1H-phenanthro[9,10d]imidazole- 2-yl)isophthalonitrile.,Neonatology. 2011;100(2):139-46. Epub 2011 Mar 2. Giroux A, et al. Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.,Bioorg Med Chem Lett. 2009 Oct 15;19(20):5837-41. Epub 2009 Aug 28. Coté B et al. Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6816-20. 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):754-6 Xu D, L,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. Epub 2008 Jun 4.