MF498
目录号 : GC16800
A selective EP4 antagonist
Cas No.:915191-42-3
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 915191-42-3 | SDF | |
| 化学名 | 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 | ||
| 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 | ||
| 分子式 | C32H33N3O7S | 分子量 | 603.7 |
| 溶解度 | ≤10mg/ml in DMSO;10mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6565 mL | 8.2823 mL | 16.5645 mL |
| 5 mM | 0.3313 mL | 1.6565 mL | 3.3129 mL |
| 10 mM | 0.1656 mL | 0.8282 mL | 1.6565 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet