A potent, selective, and orally active mPGES-1 inhibitor
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MF63

Item No. 13217

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml
λmax
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
Shipping & Storage Information
Storage
Room temperature
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    MF63 is a potent, selective, and orally active inhibitor of human mPGES-1 (IC50 = 1.3 nM).1,2 It displays greater than 1,000-fold selectivity over other prostanoid synthases.2 MF63 also potently inhibits guinea pig mPGES-1 (IC50 = 0.9 nM) but not mouse or rat mPGES-1.2 In guinea pigs or in mice expressing human mPGES-1, MF63 prevents LPS-induced pyresis, hyperalgesia, and iodoacetate-induced osteoarthritic pain.2 It does not produce the gastrointestinal toxicity that is caused by non-selective COX inhibitors, although it markedly suppresses PGE2 synthesis in the stomach.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Côté, B., Boulet, L., Brideau, C., et al. Substituted phenanthrene imidazoles as potent, selective, and orally active mPGES-1 inhibitors. Bioorg. Med. Chem. Lett. 17(24), 6816-6820 (2007).

    2. Xu, D., Rowland, S.E., Clark, P., 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. 326(3), 754-763 (2008).