Alclofenac
(Synonyms: 烯氯苯乙酸) 目录号 : GC46826
An NSAID
Cas No.:22131-79-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Alclofenac is a non-steroidal anti-inflammatory drug (NSAID) with analgesic, anti-inflammatory, and anti-pyretic properties.1,2,3 It inhibits contractions induced by serotonin (5-HT) in isolated guinea pig ileum by 28% when used at a concentration of 200 μg/ml.4 Alclofenac (480 mg/kg per day) decreases implant neutrophil and macrophage infiltration in a rat model of irritant-induced inflammation induced by implantation of heat-killed M. tuberculosis-impregnated polyurethane cubes.5
1.Delbeke, F.T., Landuyt, J., and Debackere, M.Disposition of human drug preparations in the horse. III. Orally administered alclofenacJ. Vet. Pharmacol. Ther.17(5)353-358(1994) 2.Staquet, M., Luyckx, A., and Van Cauwenberge, H.A double-blind comparison of alclofenac, pentazocine, and codeine with placebo control in pathologic painJ. Clin. Pharmacol. New Drugs11(6)450-455(1971) 3.Berry, H., Fernandes, L., Ford-Hutchinson, A.W., et al.Alclofenac and ?-penicillamine. Comparative trial in rheumatoid arthritisAnn. Rheum. Dis.37(1)93-97(1978) 4.Famaey, J.P., Fontaine, J., Seaman, I., et al.A possible role of prostaglandins in guinea-pig isolated ileum contractions to serotoninProstaglandins14(1)119-124(1977) 5.Woodland, J., Vernon-Roberts, B., Swettenham, K.V., et al.Comparison of the effects of alclofenac, flurbiprofen, and prednisolone on acute inflammatory response in the ratAnn. Rheum. Dis.36(2)160-165(1977)
| Cas No. | 22131-79-9 | SDF | |
| 别名 | 烯氯苯乙酸 | ||
| Canonical SMILES | OC(CC1=CC(Cl)=C(OCC=C)C=C1)=O | ||
| 分子式 | C11H11ClO3 | 分子量 | 226.7 |
| 溶解度 | Chloroform: soluble,Methanol: soluble | 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 | 4.4111 mL | 22.0556 mL | 44.1112 mL |
| 5 mM | 0.8822 mL | 4.4111 mL | 8.8222 mL |
| 10 mM | 0.4411 mL | 2.2056 mL | 4.4111 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。
Clinical studies on Alclofenac in the treatment of rheumatic diseases: a drug in question
Curr Med Res Opin 1975;3(5):274-85.PMID:241597DOI:10.1185/03007997509114778.
The potential advantage to patients with chronic rheumatic diseases of an effective, non-steroidal analgesic/anti-inflammatory drug which causes insignificant gastric bleeding was a decisive factor leading to the introduction of Alclofenac. Short-term double-blind trials showed that Alclofenac has analgesic/anti-inflammatory activities equivalent to phenylbutazone, indomethacin and aspirin, but superior to the fenemates and propionic acid derivatives. Long-term controlled studies, ranging from 5 months to 3-1/2 years and using reliable, objective measures revela, however, that patients with rheumatoid arthritis improve in functional status and graduate to less severe classes of disease activity, a phenomenon not observed with either indomethacin or aspirin administered to matched patients over the same periods of time. So far, clinical improvement on Alclofenac has been matched only by treatment with gold, D-penicillamine and the immunosuppressive anti-proliferative drugs. This clinical improvement on Alclofenac is reflected in haematological and serological indices, and research shows that Alclofenac, like these other antirheumatoid drugs, has a pronounced effect upon the acute-phase protein response and the extent to which L-tryptophan is bound to plasma protein. The clinical data reviewed suggest that Alclofenac represents an advance in the therapy of the rheumatic diseases.
The chemical and biological background to Alclofenac
Curr Med Res Opin 1975;3(5):241-8.PMID:241593DOI:10.1185/03007997509114774.
The essential chemistry of Alclofenac is described together with a resumé of the pharmacological and toxicological properties. Its metabolism is described and absorption and excretion commented upon. The unique character of the Alclofenac molecule in relation to its active allyloxy group and its close conformational resemblance to L-tryptophan is emphasised. Particular note is made of the absence of gastro-intestinal irritation in the long-term studies in animals and in man.
Alclofenac and D-penicillamine. Comparative trial in rheumatoid arthritis
Ann Rheum Dis 1978 Feb;37(1):93-7.PMID:24426DOI:10.1136/ard.37.1.93.
Forty-six patients with rheumatoid arthritis, 22 receiving D-penicillamine and 2j Alclofenac, took part in a 6-month single-bind external observer trial to compare the efficacy and toxicity of these drugs in the treatment of severe rheumatoid arthritis. Both drugs were active and similar in their efficacy at 6 months as judged by clinical and laboratory measurements. Penicillamine was active therapeutically by 3 months, one month before Alclofenac. 9 patients, 8 on Alclofenac and one on D-penicillamine, had to stop treatment because of lack of effect or toxic effects. Skin rashes within the first week of treatment were a major problem with Alclofenac and led to 6 withdrawals.
Alclofenac: a review of its pharmacological properties and therapeutic efficacy in rheumatoid arthritis and allied rheumatic disorders
Drugs 1977 Oct;14(4):241-59.PMID:21068DOI:10.2165/00003495-197714040-00001.
Alclofenac is a non-steroidal anti-inflammatory agent advocated for use in rheumatoid arthritis, degenerative joint disease and ankylosing spondylitis. Published data to date, suggest that Alclofenac 3g daily is comparable in efficacy with aspirin 4.8g daily, phenylbutazone 300 to 600mg daily and indomethacin 150mg daily. In Welsh patients, gastro-intestinal side-effects have generally been less frequent and milder than with the standard comparison drugs, but in other populations differences in the overall incidence of these side-effects have been less marked. Results of a long-term trial, as evidenced by alterations in certain biochemical indications of disease activity, suggest that Alclofenac may possibly reduce the severity of the disease itself, but further studies will be needed to confirm this. However, at present Alclofenac should be considered along with the other drugs of its type in the initial treatment of the arthritic patient. Skin rash is the most frequent side-effect, which in a small proportion of affected patients may be associated with systemic effects. A cutaneous reaction appears to be more likely in patients with a history of previous allergy to penicillin and other drugs.
Double-blind comparison of Alclofenac and aspirin in the treatment of rheumatoid arthritis. Part II: high dosage regime for assessment of analgesic and anti-inflammatory activity
Curr Med Res Opin 1975;3(5):309-20.PMID:241600DOI:10.1185/03007997509114781.
A double-blind trial was carried out in 76 patients with active rheumatoid arthritis to compare the analgesic and anti-inflammatory activity of 3 g. Alclofenac with 4.8 g. aspirin daily over a 6-week period. All patients selected showed reversible inflammatory swelling of the finger joints. Of the 60 patients successfully completing the trial, 30 were treated as out-patients and 30 patients received in-patient treatment for approximately the first 2 weeks. Both groups were analysed separately. Treatment was randomised and patients received the drugs in identical tablet form except for the last 16 patients who were transferred to capsules. Results showed that though the activity potential, morning stiffness, grip strength, joint pain and tenderness improved significantly at the end of the 6-week period, there was no statistical difference between the two drugs. However, functional capacity indicated slight superiority of Alclofenac over aspirin at a low level of significance. P.I.P. joint swelling showed that both in-patients and out-patients on Alclofenac improved significantly (p less than .001)compared to patients in the aspirin group. Laboratory investigations showed no difference between the two drugs as far as changes in serum proteins, serum transaminase, haemoglobin and E.S.R. levels were concerned. However, serum uric acid levels dropped significantly (.05 greater than p greater than .01) with aspirin. The incidence of side-effects was slightly higher in the aspirin group but a high incidence of skin rash (30% approx.) was recorded with Alclofenac tablets. No incidence of skin rash was recorded in patients taking Alclofenac capsules, but the number of patients taking capsules was too small to make any prediction. It appears from this study that in active rheumatoid arthritis the analgesic and anti-inflammatory activity of 3 g. Alclofenac is equivalent to 4.8 g. aspirin, and Alclofenac is superior to aspirin in reducing the inflammatory swelling of rheumatoid joints.