MF63

Microsomal prostaglandin E2 synthase-1 (mPGES-1) is the terminal enzyme in the biosynthesis of PGE2. MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM). It displays greater than 1,000-fold selectivity over other prostanoid synthases. MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1. In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain. It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.Formal Name: 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-1,3-benzenedicarbonitrile. CAS Number: 892549-43-8. Molecular Formula: C23H11ClN4. Formula Weight: 378.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml. lambdamax: 215, 255, 365 nm. SMILES: ClC1=CC2=C(C=CC=C3)C3=C(NC(C4=C(C#N)C=CC=C4C#N)=N5)C5=C2C=C1. InChi Code: 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). InChi Key: BVFLHOOKHPFDCT-UHFFFAOYSA-N.