-
-
Overview
-
Please contact us at for specific academic pricing.
Background
IC50: 0.9 and 1.3 nM for pig mPGES-1 and human mPGES-1MF63 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
-
- Properties
-
Overview
- Home
- Products
- Life Science
- Analytical Chromatography
- Assay Kits
- Biochemical Reagents
- Antibodies
- Antigens
- Enzymes
- Chemicals
- Proteins
- Liposomes
- Cell Culture
- Cell Analysis
- Cloning and Expression
- Nucleic Acid Synthesis
- Nucleic Acid Extraction
- Nucleic Acid Electrophoresis
- PCR
- Protein Gel Electrophoresis
- Protein Biochemistry
- Nanoparticles
- Glycan Analysis
- Immunohistochemistry (IHC)
- Microbiology
- Biospecimens
- Transfection Reagents
- Ion Exchange Resins
- Venoms
- Lab Solutions
- Lab Equipment
- Biosensors
- Flow Imaging Microscopes
- Fluorescence Quality Management Solutions
- Electrophoresis Systems
- Hematology Analyzers
- Isothermal Amplification Instruments
- Liquid Handling Equipment
- Luminometers
- Microfluidic Flow Control Systems
- Next-generation Sequencing Systems
- Nucleic Acid Purification Instruments
- Raman Spectroscopy Systems
- Sample Tracking Systems
- Spectrometer Accessories
- Syringe Pumps
- Thawing and Warming Systems
- Tissue Dissociation Systems
- Water Purification Systems
- Western Blotting Equipment
- General Laboratory Equipment
- Clinical Chemistry Analyzers
- Amerigo Scientific Instrument
- Automated Cell Selection Systems
- Automated Nucleic Acid Extraction Instruments
- Balances, Scales and Weighing
- Biolayer Interferometry Instruments
- Bioprocess Filtration Equipment
- Bioprocess Systems and Accessories
- Bioreactors and Fermenters
- Cappers and Decappers
- Cell Thawing Instruments
- Chromatography
- Data Loggers
- Droplet Generators
- Dry Baths
- Flow Cytometers
- Histology Laboratory Equipment
- Lab Ovens and Furnaces
- Lab Refrigeration Equipment
- Lab Shakers and Mixers
- Laboratory Centrifuges
- Laboratory Evaporators
- Laboratory Hoods
- Laboratory Incubators
- Laboratory Microscopes
- Laboratory Mills
- Laboratory Pumps
- Liquid Handling
- Live Cell Imaging Systems
- Microbiology Equipment
- Microscopy Flow Cells
- Mutation Breeding Instruments
- Oligonucleotide Synthesis Devices
- Particle Counters
- Plasma Surface Treatment Equipment
- Presses and Pellet Dies
- Surface Plasmon Resonance Instruments
- Ultrasonic Cleaners
- UV Disinfection Systems
- VOC Analysis Equipment
- VPHP Sterilization Systems
- Water Baths
- Lab Equipment
- Diagnostics & Clinical
- Applied Science
- Life Science
- Services
- About Us
- Contact Us
.
