Clonixin
(Synonyms: 氯尼辛,SCH-10304) 目录号 : GC41618
An NSAID
Cas No.:17737-65-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Clonixin is a non-steroidal anti-inflammatory drug (NSAID). It induces analgesia in rats in the formalin test when administered at doses of 80 and 120 mg/kg. It also inhibits paw edema induced by carrageenan in rats, as well as decreases vascular permeability and acts as an antipyretic in mice.
| Cas No. | 17737-65-4 | SDF | |
| 别名 | 氯尼辛,SCH-10304 | ||
| Canonical SMILES | ClC1=CC=CC(NC2=NC=CC=C2C(O)=O)=C1C | ||
| 分子式 | C13H11ClN2O2 | 分子量 | 262.7 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 25 mg/ml,Ethanol: 3.3 mg/ml | 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 | 3.8066 mL | 19.0331 mL | 38.0662 mL |
| 5 mM | 0.7613 mL | 3.8066 mL | 7.6132 mL |
| 10 mM | 0.3807 mL | 1.9033 mL | 3.8066 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。
Interaction of Clonixin with EPC liposomes used as membrane models
J Pharm Sci 2005 Jun;94(6):1277-87.PMID:15858845DOI:10.1002/jps.20351.
In this work, an overall analysis of Clonixin interaction with liposomes was achieved using different techniques, which allowed the evaluation of the change in different membrane's characteristics as well as the possible location of the drug in the membrane. Clonixin acidity constants were obtained and the values are 5.5 +/- 0.08 and 2.2 +/- 0.04. Clonixin partition coefficient (K(p)) between liposomes and water was also determined using derivative spectrophotometry, fluorescence quenching, and zeta-potential (zeta-potential). These three techniques yielded similar results. zeta-potential measurements were performed and an increase of the membrane negative charge with an increase of drug concentration was observed. Drug location within the bilayer was performed by fluorescence quenching using a set of n-(9-anthroyloxy) fatty acid probes (n = 2, 6, 9, and 12). The fluorescence intensity of all probes was quenched by the drug. This effect is more noticeable for the outer located probe, indicating that the drug is positioning in the external part of the membrane. These same probes were used for steady-state anisotropy measurements to determine the perturbation in membrane structure induced by Clonixin. Clonixin increased membrane fluidity in a concentration dependent manner, with the highest perturbation occurring nearby the 2-AS probe, closely located to the bilayer surface.
Effect of Clonixin and aspirin on platelet aggregation in human volunteers
J Clin Pharmacol 1976 Jan;16(1):30-3.PMID:1245606DOI:10.1002/j.1552-4604.1976.tb01488.x.
The effect of Clonixin and aspirin on platelet function was assessed in healthy volunteers. Both drugs inhibited secondary platelet aggregation and prolonged bleeding time, but the effect of Clonixin was significantly less than that of aspirin. Hemorrhagic complications are less likely after Clonixin than after aspirin.
Determination of Clonixin in plasma and urine by reversed-phase high-performance liquid chromatography
J Chromatogr A 2000 Aug 11;889(1-2):135-41.PMID:10985545DOI:10.1016/s0021-9673(00)00348-4.
A reversed-phase high-performance liquid chromatographic method that enables the determination of Clonixin in human plasma and urine samples is described. Recovery of the drug was over 87.6 and 80.7% for plasma and urine, respectively. The limit of quantitation of the method was established as 10 ng/ml in plasma and 20 ng/ml in urine samples, with RSDs of less than 11.1%. The applicability of the method was further assessed by determining the plasma concentrations time course of Clonixin in six healthy volunteers after single oral dose administration of 150 and 300 mg of Clonixin and Clonix.
Analgesic action of Clonixin, nifedipine and morphine using the formalin test
Gen Pharmacol 1989;20(3):319-22.PMID:2744398DOI:10.1016/0306-3623(89)90266-8.
1. The analgesic effect of ClX, nifedipine, metamizol, indoprofen and morphine in the pain induced by formalin injection (formalin test) was studied. 2. Attempts to demonstrate tolerance to ClX were unsuccessful. 3. In the analgesic test nifedipine and morphine are approximately 10 times more potent than ClX. 4. The present results suggest that the analgesic action of ClX is not mediated by mu 1, delta or kappa-opioid receptors and the anti-nociceptive effect of nifedipine may be associated with the blockade of the transmembrane inward movements of calcium.
Lack of effect of rheumatoid arthritis on Clonixin metabolism
Clin Pharmacol Ther 1975 May;17(5):622-6.PMID:1092517DOI:10.1002/cpt1975175622.
The effect of rheumatoid arthritis on the metabolism of the analgesic, 2-(3-chloro-o-toluidino) nicotinic acid (Clonixin), was evaluated in 12 patients with rheumatoid arthritis and in 12 matched healthy control subjects. Males, age-matched by decades, had no renal, gastrointestinal, or hepatic disease, and took no drugs during the study. Lower (p less than 0.02) serum albumins and higher globulins in the patients (albumin: 3.87 plus or minus 0.18; globulin: 3.14 plus or minus 0.28 gm/100 ml) than in the control subjects (albumin: 4.42 plus or minus 0.10; globulin: 2.36 plus or minus 0.08 gm/100 ml) were considered to be manifestations of rheumatoid arthritis. Fasting subjects were given single oral doses of 750 mg of Clonixin. A spectrophotometric method was used to determine drug blood levels. Serum half-life was 1.45 plus or minus 0.12 hr in patients and 1.50 plus or minus 0.13 hr in control subjects (p greater than 0.5). Mean peak concentration developed at 1.7 hr and was 40.0 plus or minus 2.6 mug/ml for patients and 46.1 plus or minus 3.1 mug/ml for control subjects. Thus a single oral dose of Clonixin results in comparable blood levels in male patients suffering from rheumatoid arthritis and in healthy control subjects.