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MF63

Chemical Structure : MF63

CAS No.: 892549-43-8

MF63 (mPGES-1 inhibitorMF63; MF-63)

Catalog No.: PC-43462Not For Human Use, Lab Use Only.

MF63 is a potent, selective, and orally active mPGES-1 inhibitor with IC50 of 1.3 nM for human mPGES-1 enzyme, >1000-fold selectivity over other prostanoid synthases.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

MF63 is a potent, selective, and orally active mPGES-1 inhibitor with IC50 of 1.3 nM for human mPGES-1 enzyme, >1000-fold selectivity over other prostanoid synthases.
MF63 strongly inhibits guinea pig mPGES-1 (IC50= 0.9 nM) but not the mouse or rat enzyme.
MF63 selectively suppresses the synthesis of PGE(2), but not other prostaglandins inhibitable by NSAIDs, yet retains NSAID-like efficacy at inhibiting LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain, relieves pyresis and pain in preclinical models of inflammation.

Physicochemical Properties

M.Wt 378.81
Formula C23H11ClN4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 43 mg/mL

Chemical Name/SMILES

1,3-Benzenedicarbonitrile, 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-

References

1. Xu D, et al. J Pharmacol Exp Ther. 2008 Sep;326(3):754-63.

2. Côté B, et al. Bioorg Med Chem Lett. 2007 Dec 15;17(24):6816-20.

3. Giroux A, et al. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5837-41.

4. Finetti F, et al. Endocr Relat Cancer. 2015 Aug;22(4):665-78.

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