Meclofenamate sodium
(Synonyms: 甲氯灭酸钠,Meclofenamate sodium) 目录号 : GC38657
A competitive inhibitor of COX-
Cas No.:6385-02-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Meclofenamate is a time-
1.Laneuville, O., Breuer, D.K., DeWitt, D.L., et al.Differential inhibition of human prostaglandin endoperoxide H synthases-1 and -2 by nonsteroidal anti-inflammatory drugsJ. Pharmacol. Exp. Ther.271(2)927-934(1994)
| Cas No. | 6385-02-0 | SDF | |
| 别名 | 甲氯灭酸钠,Meclofenamate sodium | ||
| Canonical SMILES | O=C(O[Na])C1=CC=CC=C1NC2=C(Cl)C=CC(C)=C2Cl | ||
| 分子式 | C14H10Cl2NNaO2 | 分子量 | 318.13 |
| 溶解度 | 250mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| 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 | 3.1434 mL | 15.7168 mL | 31.4337 mL |
| 5 mM | 0.6287 mL | 3.1434 mL | 6.2867 mL |
| 10 mM | 0.3143 mL | 1.5717 mL | 3.1434 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。
Pharmacology, pharmacokinetics, and therapeutic use of Meclofenamate sodium
Clin J Pain 1991;7 Suppl 1:S44-8.PMID:1810520doi
Meclofenamic acid is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). At least three different biochemical effects have been defined for meclofenamic acid. It is a potent inhibitor of the enzyme cyclooxygenase, thereby inhibiting the production of prostaglandins. It also inhibits the release of 5-HETE and LTB4 from human neutrophils stimulated with calcium ionophore and antagonizes the response of tissues to certain prostaglandins. These mechanisms may explain in part the pharmacological profile and clinical effectiveness of this compound. The rapid onset of activity of meclofenamic acid and its duration of action may be the result of its pharmacokinetic profile. Sodium meclofenamate is completely bioavailable from capsules relative to an oral suspension dosage form. Maximum meclofenamic acid plasma concentrations are achieved in 0.5-2 h following doses of capsules. Meclofenamic acid is extensively metabolized. One of the metabolites, metabolite 1, is approximately 20% as active as the parent compound in inhibiting cyclooxygenase activity in vitro. This metabolite accumulates in plasma during repeated dosing. It is possible that this metabolite may contribute to at least some of the activity observed following administration of sodium meclofenamate.
Meclofenamate sodium in the treatment of ankylosing spondylitis. Report of a European double-blind controlled multicenter study
Arzneimittelforschung 1983;33(4A):660-3.PMID:6349653doi
98 patients with reversible, definite, active ankylosing spondylitis were selected for this study. 49 patients were treated with N-(2,6-dichloro-m-tolyl)anthranilic acid, sodium salt (Meclofenamate sodium, Meclomen) and 49 patients with indometacin. Following a single-blind baseline period on placebo, patients received either 200 mg Meclofenamate sodium per day or 100 mg indometacin per day for one week, in the second week the doses were increased to 250 mg Meclofenamate sodium and 125 mg indometacin and from the third through the eight week 300 mg Meclofenamate sodium and 150 mg indometacin were given. The results of this double-blind study showed that similar improvement in mobility of the vertebral column and spondylitic pain could be achieved with Meclofenamate sodium and indometacin in patients with ankylosing spondylitis. Although both treatments were well tolerated fewer Meclofenamate sodium patients reported adverse reactions than did those who had received indometacin. It is concluded that Meclofenamate sodium offers an effective and safe alternative to indometacin in the treatment of patients with ankylosing spondylitis.
Meclofenamate sodium is an inhibitor of both the 5-lipoxygenase and cyclooxygenase pathways of the arachidonic acid cascade in vitro
Prostaglandins Leukot Med 1986 Aug;23(2-3):229-38.PMID:3020588DOI:10.1016/0262-1746(86)90190-3.
Meclofenamate sodium was compared to other nonsteroidal antiinflammatory drugs in terms of its potency to inhibit the formation of 5-HETE and LTB4 in human leukocytes and the formation of prostaglandin E2 in bovine seminal vesicles as measures of its ability to inhibit the 5-lipoxygenase and cyclooxygenase pathways of the arachidonic acid cascade. Meclofenamate sodium was about 2-4 times less potent than BW-755C in inhibiting 5-lipoxygenase enzyme activity and three times more potent than benoxaprofen, while naproxen, ibuprofen, and indomethacin showed IC50 greater than 100 microM. Meclofenamate sodium and indomethacin were the most potent inhibitors of the formation of PGE2 in bovine seminal vesicles followed by ibuprofen, naproxen, and benoxaprofen in this order. Meclofenamate sodium, like BW-755C, can be considered a dual inhibitor of 5-lipoxygenase and cyclooxygenase pathways of arachidonic acid cascade. This finding may explain in part the antiinflammatory activity of Meclofenamate sodium.
Double-blind comparison of Meclofenamate sodium plus codeine, Meclofenamate sodium, codeine, and placebo for relief of pain following surgical removal of third molars
J Oral Maxillofac Surg 1990 Aug;48(8):785-90.PMID:2197381DOI:10.1016/0278-2391(90)90332-v.
A single-dose, randomized, double-blind, parallel-treatment study was performed in 200 outpatients with acute pain caused by the surgical removal of impacted third molars. Meclofenamate 100 mg plus codeine 60 mg, meclofenamate 50 mg plus codeine 30 mg, meclofenamate 100 mg, codeine 60 mg, and placebo treatment groups were compared for sum of pain intensity differences, peak pain intensity difference, sum of pain relief scores, peak pain relief, number of observations at which pain was half relieved, overall evaluation of effectiveness, and time to remedication with a backup analgesic. Meclofenamate 100 mg plus codeine 60 mg was significantly more effective (P less than .005) than codeine 60 mg for all variables except number of observations at which pain was half relieved. Both meclofenamate-codeine combinations and meclofenamate 100 mg alone were significantly more effective (P less than .005) than placebo for all variables. Eleven adverse experiences were reported in 7 patients (3.5%); the most common was somnolence in 1 patient receiving meclofenamate 100 mg plus codeine 60 mg, in 2 treated with meclofenamate 50 mg plus codeine 30 mg, and in 1 treated with codeine 60 mg.
Analgesic efficacy of Meclofenamate sodium in episiotomy pain
Pharmacotherapy 1986 Sep-Oct;6(5):205-10.PMID:3540870DOI:10.1002/j.1875-9114.1986.tb03478.x.
Meclofenamate sodium was compared, double-blind, with codeine and placebo for the treatment of acute episiotomy pain. One hundred sixty-eight women with moderate or severe episiotomy pain after normal delivery were assigned randomly to one of four treatment groups: one received Meclofenamate sodium 200 mg at dose 1 and 100 mg at doses 2 and 3; one received Meclofenamate sodium 100 mg at dose 1 and 50 mg at doses 2 and 3; one received codeine 60 mg at all three doses; and one received placebo at all three doses. Efficacy measurements were evaluated periodically for 6 hours after medication. After the first administration, both doses of Meclofenamate sodium were significantly superior to placebo and to codeine from 2-6 hours in pain intensity difference and pain relief. For second and third doses, data were available for too few patients to allow valid analysis and interpretation. Adverse effects occurred in 4 patients in each Meclofenamate sodium group, and in 8 in the codeine group and in 6 in the placebo group. The study indicates that single 100- and 200-mg doses of Meclofenamate sodium are as safe as, and significantly more effective than, codeine 60 mg or placebo for episiotomy pain.