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MF498
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MF498图片
CAS NO:915191-42-3
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt603.7
Cas No.915191-42-3
FormulaC32H33N3O7S
Solubility≤10mg/ml in DMSO;10mg/ml in dimethyl formamide
Chemical NameN-[[[4-(5,9-diethoxy-6,8-dihydro-6-oxo-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylphenyl]methyl]sulfonyl]-2-methoxy-benzeneacetamide
Canonical SMILESO=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
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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.