WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522527
Description: MF-63 is a novel and selective mPGES-1 inhibitor. MF63 potently inhibited the human mPGES-1 enzyme (IC(50) = 1.3 nM), with a high degree (>1000-fold) of selectivity over other prostanoid synthases. In rodent species, MF63 strongly inhibited guinea pig mPGES-1 (IC(50) = 0.9 nM) but not the mouse or rat enzyme. MF63 did not cause NSAID-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the KI mice or nonhuman primates, although it markedly inhibited PGE(2) synthesis in the KI mouse stomach.
MedKoo Cat#: 522527
Chemical Formula: C23H11ClN4
Exact Mass: 378.0672
Molecular Weight: 378.82
Elemental Analysis: C, 72.92; H, 2.93; Cl, 9.36; N, 14.79
Synonym: MF-63; MF63; MF 63
IUPAC/Chemical Name: 2-(6-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)-isophthalonitrile
InChi Key: BVFLHOOKHPFDCT-UHFFFAOYSA-N
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)
SMILES Code: N#CC1=CC=CC(C#N)=C1C2=NC3=C4C=CC(Cl)=CC4=C5C=CC=CC5=C3N2
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 378.82 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Xu D, Rowland SE, Clark P, Giroux A, Côté B, Guiral S, Salem M, Ducharme Y,
Friesen RW, Méthot N, Mancini J, Audoly L, Riendeau D. 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.
doi: 10.1124/jpet.108.138776. Epub 2008 Jun 4. PubMed PMID: 18524979.
Microsomal prostaglandin E synthase-1 (mPGES-1) is a terminal prostaglandin E(2) (PGE(2)) synthase in the cyclooxygenase pathway. Inhibitors of mPGES-1 may block PGE(2) production and relieve inflammatory symptoms.