5-Acetylsalicylic acid
(Synonyms: 5-乙酰基水杨酸) 目录号 : GC38687
5-Acetylsalicylic acid (5-acetyl-2-hydroxybenzoic acid) is a nonsteroidal anti-inflammatory drug.
Cas No.:13110-96-8
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
5-Acetylsalicylic acid (5-acetyl-2-hydroxybenzoic acid) is a nonsteroidal anti-inflammatory drug.
5-Acetylsalicylic acid (5-ASA) is initially shown to downregulate the inducible cyclooxygenase/prostaglandin E2 (COX-2/PGE2) signalling in mucosa inflammatory cells. Generally 5-ASA decreases the nuclear factor κB (NF-κB) activity induced by TNF-α, modulating the NF-κB inhibitor, IκBα, as well as the NF-κB transcriptional activity induced by IL-1, although it does prevent neither IL-1-induced IκBα degradation nor IL-1-induced nuclear translocation of NF-κB family members. 5-ASA is also found to increase β-catenin expression/phosphorylation and the expression of μ-protocadherin in intestine cells while reducing the expression of Wnt/β-catenin target genes and the activity of the protein phosphatase 2A. 5-ASA enhances PPAR-γ expression/activity in intestine cells and promotes its translocation from the cytoplasm to the nucleus -- this is followed by the induction of the tumour suppressor gene PTEN, the activation of caspases 8 and 3, and the inhibition of antiapoptotic proteins. It induces membranous expression of E-cadherin and increases cell adhesion through inhibition of p-21 activated kinase-1 and modulation of N-glycosylation; Also interferes with the mitogen activated protein kinase and phosphatidylinositol-4,5-bisphosphate 3-kinase/Akt pathways[1].
5-ASA is rapidly adsorbed and extensively acetylated to N-acetyl-5-ASA by the N-acetyltransferase 1 enzyme in intestinal epithelial cells and the liver. It is generally well tolerated and the most common side effects include headache, nausea, and abdominal pain[1].
[1] Cristiana Perrotta, et al. Gastroenterology Research and Practice. 2015.
| Cas No. | 13110-96-8 | SDF | |
| 别名 | 5-乙酰基水杨酸 | ||
| Canonical SMILES | O=C(O)C1=CC(C(C)=O)=CC=C1O | ||
| 分子式 | C9H8O4 | 分子量 | 180.16 |
| 溶解度 | DMSO : 100 mg/mL (555.06 mM; Need ultrasonic) | 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 | 5.5506 mL | 27.7531 mL | 55.5062 mL |
| 5 mM | 1.1101 mL | 5.5506 mL | 11.1012 mL |
| 10 mM | 0.5551 mL | 2.7753 mL | 5.5506 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。
From Solution Studies of Pharmaceuticals (Aspirin and Related Compounds) to the Thermodynamics of Aspirin-β-Cyclodextrin Interaction in water and N,N-Dimethylformamide
Int J Mol Sci 2022 Oct 4;23(19):11750.PMID:36233049DOI:10.3390/ijms231911750.
The solution behavior of pharmaceuticals (acetylsalicylic acid, 4-acetoxybenzoic acid and 5-Acetylsalicylic acid) in water and N,N-Dimethylformamide (DMF) at 298.15 K were investigated through solubility, conductance and calorimetric measurements. Taking into account the formation of ion pairs of these pharmaceuticals in water, the solution Gibbs energies of the dissociated electrolytes in this solvent were calculated. Thus, the solution thermodynamics of these compounds in water are reported using enthalpy data obtained by calorimetry. These pharmaceuticals undergo solvation when exposed to a saturated atmosphere of DMF. As the composition of the solid is not the same as that in solution, the Gibbs energy of the solutions of these compounds could not be obtained; only enthalpy data are reported. The thermodynamics of the interaction of acetylsalicylic acid (aspirin) with β-cyclodextrin in water and DMF is fully discussed, emphasizing the two different processes that take place in water at the two different pHs. In all cases, the favorable Gibbs energies for these processes are entropically controlled, mainly resulting from the higher dehydration/desolvation that the receptor undergoes upon interaction with the guest.
Clinical perspectives--biologics in IBD: What's all the fuss?
Can J Gastroenterol 2001 Dec;15(12):799-804.PMID:11773946DOI:10.1155/2001/605398.
Up until the present time, agents with relatively nonspecific anti-inflammatory or immunomodulatory effects such as 5-Acetylsalicylic acid, corticosteroids and azathioprine have been the mainstay of inflammatory bowel disease medical therapy. These drugs have been quite useful in one or more clinical settings, but they have been hampered by modest efficacy, significant toxicity or both. With greater understanding of the specific pathways of the gut mucosal immune response, it is hoped that newer biologic response modifiers will provide better efficacy, with an improved adverse event profile compared with older existing therapies. This article examines the evidence behind the use of biologic therapies such as anti-tumour necrosis factor-alpha, interleukin-10, interleukin-11, anti-integrin antibody and antisense intercellular adhesion molecule-1 oligonucleotide.
Polymyositis associated with ulcerative colitis
Gut 1993 Apr;34(4):567-9.PMID:8491410DOI:10.1136/gut.34.4.567.
An elderly woman with chronic ulcerative colitis who developed proximal muscle weakness, increased serum creatine phosphokinase activity, and histological and electromyographic abnormalities characteristic of polymyositis is described. Treatment with corticosteroids and 5-Acetylsalicylic acid was followed by a remission in bowel symptoms, improvement in muscle power, and reversal of electromyographic changes. An autoimmune link between the two disorders seems likely.
Treatment of spondyloarthropathy with 5-aminosalicylic acid (mesalazine): an open trial
J Rheumatol 2000 Mar;27(3):723-6.PMID:10743816doi
Objective: Ankylosing spondylitis (AS) and spondyloarthropathy (SpA) are inflammatory diseases of unknown etiology. Various exogenous and endogenous (inherited) factors play a role in their development. Sulfasalazine (SSZ) is generally accepted as a disease modifying drug in the treatment of AS and SpA. Which part of SSZ, 5-Acetylsalicylic acid (5-ASA, mesalazine) or sulfapyridine (SP), is the effective moiety is unknown. As the bowel, colon, and the ileum play an important role in the development of AS and SpA, it may be possible that 5-ASA is the effective moiety, with a similar mode of action as in the treatment of inflammatory bowel disease. To determine the efficacy of 5-ASA an open pilot study was done in 2 groups of patients with SpA. Methods: Twenty patients with SpA, who were taking SSZ, were switched to 5-ASA (Pentasa), and 19 patients with active SpA were treated with 5-ASA without previous administration of SSZ. Results: In the first group, 17 (85%) patients responded with respect to the physician global clinical assessment compared to the previous SSZ treatment period; whereas in the second patient group a statistically significant improvement was obtained in erythrocyte sedimentation rate. Conclusion: The results support our hypothesis that 5-ASA might be the active moiety of SSZ in the treatment of SpA.
Steroid therapy for inflammatory bowel disease
Nihon Rinsho 2017 Mar;75(3):398-402.PMID:30566781doi
In inflammatory bowel disease (IBD) as represented by ulcerative colitis (UC) and Crohn's disease (CD), UC is characterized by the diffuse inflammation from rectum and the resulting frequent diarrhea and bloody stool, and CD is characterized by scattered inflammation that may affect any part of the gastrointestinal tract from mouth to anus. Both diseases include diarrhea and abdominal cramping or pain, therefore IBD patients lose the quality of life coclusively. In general, salazosulfapyridine and 5-Acetylsalicylic acid (5-ASA) are baseline drugs for IBD, but sometimes these drugs are insufficient to suppress their inflammation. Steroid therapy is chosen as an induction treatment at that situation but not as a maintenance therapy. In this session, I would like to show how to use steroid and what are side effects of steroid for the treatment of IBD.