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MF63

Catalog No.GC11743

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

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MF63 Chemical Structure

Cas No.: 892549-43-8

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1mg
$33.00
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5mg
$99.00
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10mg
$162.00
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25mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

IC50: 0.9 and 1.3 nM for pig mPGES-1 and human mPGES-1

MF63 is a potent, selective and orally active mPGES-1 inhibitor. Microsomal prostaglandin E synthase-1 (mPGES-1) is a terminal prostaglandin E2 synthase in the cyclooxygenase pathway. Thus, inhibitors of mPGES-1 may block prostaglandin E2 production and relieve inflammatory symptoms.

In vitro: MF63 was found to be significantly more potent than those previously reported mPGES-1 inhibitors with an intrinsic inhibitory potency on the recombinant human mPGES-1 enzyme. Furthermore, MF63 showed a PGE2 whole cell inhibition in A549 cells and a human whole blood activity [1].

In vivo: In rodent species, MF63 inhibited guinea pig mPGES-1 strongly but not the mouse or rat enzyme. When tested in the guinea pig and a knock-in (KI) mouse expressing human mPGES-1, MF63 suppressed the synthesis of PGE2 selectively, but not other prostaglandins that were inhibitable by nonsteroidal anti-inflammatory drugs (NSAID), yet remaided NSAID-like efficacy at inhibiting lipopolysaccharide-induced hyperalgesia, pyresis, and iodoacetate-induced osteoarthritic pain. Additionally, MF63 did not cause NSAID-like gastrointestinal toxic effects, such as mucosal erosions or leakage in the KI mice or nonhuman primates, although MF63 markedly inhibited PGE2 synthesis in the KI mouse stomach [1].

Clinical trial: N/A

Reference:
[1] Xu D,Rowland SE,Clark P,Giroux A,Cté 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.

Chemical Properties

Cas No. 892549-43-8 SDF
Chemical Name 2-(9-chloro-1H-phenanthro[9,10-d]imidazol-2-yl)isophthalonitrile
Canonical SMILES ClC1=CC(C2=CC=CC=C2C3=C4NC(C5=C(C#N)C=CC=C5C#N)=N3)=C4C=C1
Formula C23H11ClN4 M.Wt 378.81
Solubility DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.3 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6398 mL 13.1992 mL 26.3985 mL
5 mM 0.528 mL 2.6398 mL 5.2797 mL
10 mM 0.264 mL 1.3199 mL 2.6398 mL
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Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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