Fenoprofen
(Synonyms: 3-(4-苯氧基苯基)丙酸,LILLY-53858) 目录号 : GC64525
An NSAID
Cas No.:29679-58-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Fenoprofen is a non-steroidal anti-inflammatory drug (NSAID).1 It inhibits spontaneous and estradiol-stimulated prostaglandin F2α release by 84% in isolated rat uterine horns when used at a concentration of 33 μM. Fenoprofen (10 mg/kg, i.p.) reduces serum PGF2α levels in rats. It reduces acetic acid-induced writhing and stretching as well as formalin-induced licking behaviors, indicating analgesic activity, however, it also induces formation of gastric lesions in mice, a common adverse effect associated with NSAID administration.2
1.Patrono, C., Ciabattoni, G., and Grossi-Belloni, D.In vitro and in vivo inhibition of prostaglandin synthesis by fenoprofen, a non steroid anti-inflammatory drugPharmacol. Res. Commun.6(5)509-518(1974) 2.Agotegaray, M., Gumilar, F., Boeris, M., et al.Enhanced analgesic properties and reduced ulcerogenic effect of a mononuclear copper(II) complex with fenoprofen in comparison to the parent drug: Promising insights in the treatment of chronic inflammatory diseasesBiomed. Res. Int.2014(2014)
| Cas No. | 29679-58-1 | SDF | Download SDF |
| 别名 | 3-(4-苯氧基苯基)丙酸,LILLY-53858 | ||
| 分子式 | C15H14O3 | 分子量 | 242.27 |
| 溶解度 | DMSO : 100 mg/mL (412.76 mM; Need ultrasonic) | 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 | 4.1276 mL | 20.6381 mL | 41.2763 mL |
| 5 mM | 0.8255 mL | 4.1276 mL | 8.2553 mL |
| 10 mM | 0.4128 mL | 2.0638 mL | 4.1276 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。
Ibuprofen
Ann Intern Med 1979 Dec;91(6):877-82.PMID:391117DOI:10.7326/0003-4819-91-6-877.
Ibuprofen was introduced in England in 1967 and in the United States in 1974 as an anti-inflammatory drug in humans. It has weak but definite anti-inflammatory properties similar to those of aspirin, milligram for milligram, but with considerably less adverse effect on the stomach. Ibuprofen is chemically related to Fenoprofen and naproxen, but lack of effect for any one in this chemical class of propionic-acid derivatives does not necessarily mean lack of effect for any other in an individual patient. The drug has analgesic properties, probably related to its anti-inflammatory effect. It inhibits prostaglandin synthesis and has no effect on the adrenopituitary axis, making it a nonsteroidal agent. Ibuprofen has been shown to be effective in rheumatoid arthritis and osteoarthritis and is probably effective in ankylosing spondylitis, gout, and Bartter's syndrome.
Single dose oral Fenoprofen for acute postoperative pain in adults
Cochrane Database Syst Rev 2011 Feb 16;2011(2):CD007556.PMID:21328296DOI:10.1002/14651858.CD007556.pub2.
Background: Fenoprofen is a non-steroidal anti-inflammatory drug (NSAID), available in several different countries, but not widely used. Objectives: To assess the efficacy of single dose oral Fenoprofen in acute postoperative pain, and associated adverse events. Search strategy: We searched Cochrane CENTRAL, MEDLINE, EMBASE and the Oxford Pain Relief Database for studies to December 2010. Selection criteria: Single oral dose, randomised, double-blind, placebo-controlled trials of Fenoprofen for relief of established moderate to severe postoperative pain in adults. Data collection and analysis: Studies were assessed for methodological quality and data extracted by two review authors independently. Summed total pain relief (TOTPAR) or pain intensity difference (SPID) over 4 to 6 hours was used to calculate the number of participants achieving at least 50% pain relief. These derived results were used to calculate, with 95% confidence intervals, the relative benefit compared to placebo, and the number needed to treat (NNT) for one participant to experience at least 50% pain relief over 4 to 6 hours. Numbers of participants using rescue medication over specified time periods, and time to use of rescue medication, were sought as additional measures of efficacy. Information on adverse events and withdrawals was collected. Main results: Five studies (696 participants) met the inclusion criteria; 24 participants were treated with Fenoprofen 12.5 mg, 23 with Fenoprofen 25 mg, 79 with Fenoprofen 50 mg, 78 with Fenoprofen 100 mg, 146 with Fenoprofen 200 mg, 55 with Fenoprofen 300 mg, 43 with zomepirac 100 mg, 30 with morphine 8 mg, 77 with codeine 60 mg, and 141 with placebo. Participants had pain following third molar extraction, laparoscopy, minor day surgery and episiotomy. The NNT for at least 50% pain relief over 4 to 6 hours with a single dose of Fenoprofen 200 mg compared to placebo was 2.3 (1.9 to 3.0). There were insufficient data to analyse other doses or active comparators, time to use of rescue medication, or numbers of participants needing rescue medication. There was no difference in numbers of participants experiencing any adverse events between Fenoprofen 200 mg and placebo. No serious adverse events or adverse event withdrawals were reported in these studies. Authors' conclusions: Oral Fenoprofen 200 mg is effective at treating moderate to severe acute postoperative pain, based on limited data for at least 50% pain relief over 4 to 6 hours. Efficacy of other doses, other efficacy outcomes, and safety and tolerability could not be assessed.
Carborane Analogues of Fenoprofen Exhibit Improved Antitumor Activity
ChemMedChem 2023 Mar 1;18(5):e202200583.PMID:36583943DOI:10.1002/cmdc.202200583.
Fenoprofen is a widely used nonsteroidal anti-inflammatory drug (NSAID) against rheumatoid arthritis, degenerative joint disease, ankylosing spondylitis and gout. Like other NSAIDs, Fenoprofen inhibits the synthesis of prostaglandins by blocking both cyclooxygenase (COX) isoforms, COX-1 the "house-keeping" enzyme and COX-2 the induced isoform from pathological stimuli. Unselective inhibition of both COX isoforms results in many side effects, but off-target effects have also been reported. The steric modifications of the drugs could afford the desired COX-2 selectivity. Furthermore, NSAIDs have shown promising cytotoxic properties. The structural modification of Fenoprofen using bulky dicarba-closo-dodecaborane(12) (carborane) clusters and the biological evaluation of the carborane analogues for COX inhibition and antitumor potential showed that the carborane analogues exhibit stronger antitumor potential compared to their respective aryl-based compounds.
Evidence-based guideline update: NSAIDs and other complementary treatments for episodic migraine prevention in adults: report of the Quality Standards Subcommittee of the American Academy of Neurology and the American Headache Society
Neurology 2012 Apr 24;78(17):1346-53.PMID:22529203DOI:10.1212/WNL.0b013e3182535d0c.
Objective: To provide updated evidence-based recommendations for the preventive treatment of migraine headache. The clinical question addressed was: Are nonsteroidal anti-inflammatory drugs (NSAIDs) or other complementary treatments effective for migraine prevention? Methods: The authors analyzed published studies from June 1999 to May 2009 using a structured review process to classify the evidence relative to the efficacy of various medications for migraine prevention. Results: The author panel reviewed 284 abstracts, which ultimately yielded 49 Class I or Class II articles on migraine prevention; of these 49, 15 were classified as involving nontraditional therapies, NSAIDs, and other complementary therapies that are reviewed herein. Recommendations: Petasites (butterbur) is effective for migraine prevention and should be offered to patients with migraine to reduce the frequency and severity of migraine attacks (Level A). Fenoprofen, ibuprofen, ketoprofen, naproxen, naproxen sodium, MIG-99 (feverfew), magnesium, riboflavin, and subcutaneous histamine are probably effective for migraine prevention (Level B). Treatments considered possibly effective are cyproheptadine, Co-Q10, estrogen, mefenamic acid, and flurbiprofen (Level C). Data are conflicting or inadequate to support or refute use of aspirin, indomethacin, omega-3, or hyperbaric oxygen for migraine prevention. Montelukast is established as probably ineffective for migraine prevention (Level B).
Fenoprofen and codeine analgesia
Clin Pharmacol Ther 1981 May;29(5):606-16.PMID:7214791DOI:10.1038/clpt.1981.85.
Studies were conducted on postpartum and postoperative patients to estimate the dose-response line of Fenoprofen and to contrast it with codeine and placebo. The postpartum patients included women with episiotomy pain and with uterine cramping. This mix allowed contrast of ability of the various pain models to distinguish codeine from placebo. The methodology for the studies was single-dose parallel groups design with interviews conducted by trained nurse observers to obtain subjective responses. More than 850 patients participated in the trial. The results indicate that Fenoprofen at doses as low as 12.5 mg has analgesic properties. In each of the five studies, the mean value of 100- and/or 200-mg doses of Fenoprofen for the variable sum of the pain intensity difference (SPID) was higher than that of 65 mg codeine. The pooled relative potency calculation based on SPID suggests that 100 mg Fenoprofen is approximately equivalent to 60 mg codeine. In their ability to distinguish codeine from placebo, patients with uterine cramp, episiotomy, or surgical pain did not appear to differ.