Apyramide
目录号 : GC31850
Apyramide是一种抗炎药物。
Cas No.:68483-33-0
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
Apyramide is an anti-inflammatory agent.
Apyramide is far less toxic than indomethacin in rats and mice by the oral or the i.p. route. It exhibits anti-inflammatory activity on carrageenin-induced paw oedema, cotton pellet granuloma and adjuvant arthritis, as well as analgesic and antipyretic activities[1].
[1]. Sauvaire D, et al. Pharmacological activity and toxicity of apyramide: comparison with non-steroidal anti-inflammatory agents. Drugs Exp Clin Res. 1987;13(5):247-52.
| Cas No. | 68483-33-0 | SDF | |
| Canonical SMILES | O=C(OC1=CC=C(NC(C)=O)C=C1)CC2=C(C)N(C(C3=CC=C(Cl)C=C3)=O)C4=C2C=C(OC)C=C4 | ||
| 分子式 | C27H23ClN2O5 | 分子量 | 490.93 |
| 溶解度 | Soluble in DMSO | 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 | 2.037 mL | 10.1848 mL | 20.3695 mL |
| 5 mM | 0.4074 mL | 2.037 mL | 4.0739 mL |
| 10 mM | 0.2037 mL | 1.0185 mL | 2.037 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。
Pharmacokinetics of an indomethacin pro-drug: apyramide after intravenous administration in dog
The pharmacokinetics of apyramide, an ester of indomethacin and acetaminophen (paracetamol), were determined after intravenous administration to nine beagle dogs. Indomethacin and its pro-drug, apyramide, were extracted from acetonitrile-precipitated plasma by a solvent-demixing procedure and the concentration of these two drugs was measured by a reversed-phase liquid chromatographic assay. The kinetic evolution with time of plasma levels of apyramide and of indomethacin resulting from enzymatic hydrolysis was compared with values obtained for indomethacin injected in equimolar dose. Plasma levels of apyramide quickly decreased and the mean (+/- SD) half life was 0.15 +/- 0.08 h. For metabolic indomethacin, the mean (+/- SD) area under curve was 12.36 +/- 4.80 mg.h/l and the mean (+/- SD) half life of terminal phase was 16.71 +/- 9.46 h. After administration of indomethacin, these values were 17.60 +/- 4.12 mg.h/l and 7.89 +/- 2.20 h, respectively.
Pharmacological activity and toxicity of apyramide: comparison with non-steroidal anti-inflammatory agents
An experimental and comparative study was conducted on 1-(p-chlorobenzoyl)-2-methyl-5-methoxyindole-3-p-acetamidophenol acetate (Apyramide) and known anti-inflammatory agents. Apyramide was far less toxic than indomethacin in rats and mice by the oral or the i.p. route. It exhibited anti-inflammatory activity on carrageenin-induced paw oedema, cotton pellet granuloma and adjuvant arthritis, as well as analgesic and antipyretic activities. The acute ulcerogenic effect of Apyramide was lower than that of indomethacin.