Carprofen
(Synonyms: 卡洛芬) 目录号 : GC17341
An NSAID used in animals
Cas No.:53716-49-7
Sample solution is provided at 25 µL, 10mM.
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Carprofen is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively.
Carprofen (Compound 1) is a nonsteroid anti-inflammatory agent, acts as a multi-target FAAH/COX inhibitor, with IC50s of 3.9 μM, 22.3 μM and 78.6 μM for COX-2, COX-1 and FAAH, respectively[1]. Carprofen (10 µg/mL) shows cytoprotective effects in CCL and CaCL cells and decreases apoptosis of both cells. Carprofen (10 µg/mL) exhibits nonsignificant increase in PGE2 concentration, compared with that of the respective CCL or CaCL controls[2].
Carprofen (2.2 mg/kg, p.o.) significantly decreases PGE2 concentration in blood of dogs on days 3 and 10. Carprofen also decreases amounts of gastric PGE2 synthesis on day 3, but the inhibition is not obvious on day 10. In addition, Carprofen shows no activity against gastric PGE1 synthesis in dogs on day 3 and 10[3].
References:
[1]. Favia AD, et al. Identification and characterization of carprofen as a multitarget fatty acid amide hydrolase/cyclooxygenase inhibitor. J Med Chem. 2012 Oct 25;55(20):8807-26.
[2]. Waldherr K, et al. In vitro cytoprotective effects of acetylsalicylic acid, carprofen, meloxicam, or robenacoxib against apoptosis induced by sodium nitroprusside in canine cruciate ligament cells. Am J Vet Res. 2012 Nov;73(11):1752-8.
[3]. Sessions JK, et al. In vivo effects of carprofen, deracoxib, and etodolac on prostanoid production in blood, gastric mucosa, and synovial fluid in dogs with chronic osteoarthritis. Am J Vet Res. 2005 May;66(5):812-7.
| Cell experiment [1]: | |
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Cell lines |
gastric mucosa |
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Preparation method |
The solubility of this compound in DMSO is >11.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
40 or 400 μg/mL |
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Applications |
In the gastric mucosa of dogs, carprofen increased in vitro conductance and permeability to mannitol. Carprofen (400 μg/mL) caused sloughing of epithelial cells. Carprofen appeared to compromise gastric mucosal integrity and barrier function in dogs. |
| Animal experiment [2]: | |
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Animal models |
Dogs with chronic unilateral osteoarthritis of the stifle joint |
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Dosage form |
10 days with a 30- to 60-day washout period |
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Application |
Carprofen significantly suppressed PGE2 concentrations in blood at days 3 and 10. Carprofen significantly decreased gastric synthesis of PGE2 at day 3 but not day 10 of each treatment period. Carprofen decreased synovial fluid PGE2 concentrations in the affected and unaffected stifle joints at days 3 and 10. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Hicks M A, Hosgood G L, Morgan T W, et al. In vitro effect of carprofen and meloxicam on the conductance and permeability to mannitol and the histologic appearance of the gastric mucosa of dogs[J]. American journal of veterinary research, 2011, 72(4): 570-577. [2] Sessions J K, Reynolds L R, Budsberg S C. In vivo effects of carprofen, deracoxib, and etodolac on prostanoid production in blood, gastric mucosa, and synovial fluid in dogs with chronic osteoarthritis[J]. American journal of veterinary research, 2005, 66(5): 812-817. | |
| Cas No. | 53716-49-7 | SDF | |
| 别名 | 卡洛芬 | ||
| 化学名 | 2-(6-chloro-9H-carbazol-2-yl)propanoic acid | ||
| Canonical SMILES | CC(C1=CC2=C(C=C1)C3=C(N2)C=CC(=C3)Cl)C(=O)O | ||
| 分子式 | C15 H12ClNO2 | 分子量 | 273.71 |
| 溶解度 | ≥ 11.05mg/mL 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6535 mL | 18.2675 mL | 36.535 mL |
| 5 mM | 0.7307 mL | 3.6535 mL | 7.307 mL |
| 10 mM | 0.3654 mL | 1.8268 mL | 3.6535 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet