MF498
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
MF498 is a novel and selective EP4 antagonist [1].
Prostaglandin E2 receptors (EP) are G-protein coupled receptors (GPCRs) and functions with the binding of Prostaglandin (PG) E2. The EPs exhibit differences in signal transduction, tissue localization, and regulation of expression. The EP4 receptor is over-expressed in human prostate cancer tissue [2].
In vitro: MF498 was a selective EP4 receptor antagonist with the Ki of 0.7 nM while the Ki > 1 μM for other EP receptors. In HEK293 cells expressing human EP4 receptor, MF498 inhibited EP ligand-induced activity with an IC50 value of 1.7 nM [1].
In vivo: In rodent models of rheumatoid and osteoarthritis, MF498 inhibited inflammation without gastrointestinal toxicity, the ED50 values was as low as 0.02 mg/kg/day[1].In adjuvant-induced arthritis (AIA) rat model for rheumatoid arthritis (RA), MF498 inhibited inflammation. In addition, MF498 was effective in relieving OA-like pain in guinea pigs. In rat models of gastrointestinal toxicity, MF498 was well tolerated, causing no mucosal leakage or erosions. In a furosemide-induced diuresis model, MF498 reduced furosemide-induced natriuresis by 50% [3].
References:
[1] P. Clark, S. E. Rowland, D. Denis, et al. MF498 [N-{[4-(5,9-diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.Journal of Pharmacology and Experimental Therapeutics 325(2), 425-434 (2008).
[2] Sugimoto Y, Narumiya S. Prostaglandin E receptors[J]. Journal of Biological Chemistry, 2007, 282(16): 11613-11617.
[3] Clark P, Rowland S E, Denis D, et al. MF498 [N-{[4-(5, 9-Diethoxy-6-oxo-6, 8-dihydro-7H-pyrrolo [3, 4-g] quinolin-7-yl)-3-methylbenzyl] sulfonyl}-2-(2-methoxyphenyl) acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis[J]. Journal of Pharmacology and Experimental Therapeutics, 2008, 325(2): 425-434.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 603.7 |
Cas No. | 915191-42-3 |
Formula | C32H33N3O7S |
Solubility | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide |
Chemical Name | N-[[[4-(5,9-diethoxy-6,8-dihydro-6-oxo-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methyl]sulfonyl]-2-methoxy-benzeneacetamide |
SDF | Download SDF |
Canonical SMILES | O=C1N(C2=C(C)C=C(CS(NC(CC3=CC=CC=C3OC)=O)(=O)=O)C=C2)CC4=C(OCC)C5=C(C=CC=N5)C(OCC)=C41 |
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