Pentoxifylline
(Synonyms: NSC 637086, Oxpentifylline) 目录号 : GC40685
Pentoxifylline is a methylxanthine derivative.
Cas No.:6493-05-6
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
Pentoxifylline is a competitive nonselective phosphodiesterase inhibitor.Target: PDEPentoxifylline is a competitive nonselective phosphodiesterase inhibitor which raises intracellular cAMP, activates PKA, inhibits TNF and leukotriene synthesis, and reduces inflammation and innate immunity. In addition, pentoxifylline improves red blood cell deformability, reduces blood viscosity and decreases the potential for platelet aggregation and thrombus formation. Pentoxifylline is also an antagonist at adenosine 2 receptors [1]. Pentoxifylline is generally well tolerated. Based on the totality of the available evidence, it is possible that pentoxifylline could have a place in the treatment of IC as a means of improving walking distance and as a complimentary treatment assuming all other essential measures such as lifestyle change, exercise and treatment for secondary prevention have been taken into account [2]. Pentoxifylline reduce AST and ALT levels and may improve liver histological scores in patients with NALFD/NASH, but did not appear to affect cytokines. Large, prospective, and well-designed randomized, controlled studies are needed to address this issue [3].
References:
[1]. http://en.wikipedia.org/wiki/Pentoxifylline
[2]. Salhiyyah, K., et al., Pentoxifylline for intermittent claudication. Cochrane Database Syst Rev, 2012. 1: p. CD005262.
[3]. Li, W., et al., Systematic review on the treatment of pentoxifylline in patients with non-alcoholic fatty liver disease. Lipids Health Dis, 2011. 10: p. 49.
| Cas No. | 6493-05-6 | SDF | |
| 别名 | NSC 637086, Oxpentifylline | ||
| Canonical SMILES | CC(CCCCN1C(N(C)C(N=CN2C)=C2C1=O)=O)=O | ||
| 分子式 | C13H18N4O3 | 分子量 | 278.3 |
| 溶解度 | DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 2 mg/ml,PBS (pH 7.2): 1 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 | 3.5932 mL | 17.9662 mL | 35.9324 mL |
| 5 mM | 0.7186 mL | 3.5932 mL | 7.1865 mL |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5932 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。
Pentoxifylline
J Am Acad Dermatol 1994 Apr;30(4):603-21.PMID:8157787DOI:10.1016/s0190-9622(94)70069-9.
Pentoxifylline (oxpentifylline) is a methylxanthine derivative with potent hemorrheologic properties. In the United States it is marketed for the treatment of intermittent claudication. Human and animal studies have shown that Pentoxifylline therapy results in a variety of physiological changes at the cellular level, which may be important in treating a diverse group of human afflictions. Immune modulation includes increased leukocyte deformability and chemotaxis, decreased endothelial leukocyte adhesion, decreased neutrophil degranulation and release of superoxides, decreased production of monocyte-derived tumor necrosis factor, decreased leukocyte responsiveness to interleukin 1 and tumor necrosis factor, inhibition of T and B lymphocyte activation, and decreased natural killer cell activity. Hypercoagulable states improve through decreased platelet aggregation and adhesion, increased plasminogen activator, increased plasmin, increased antithrombin III, decreased fibrinogen, decreased alpha 2-antiplasmin, decreased alpha 1-antitrypsin, and decreased alpha 2-macroglobulin. Wound healing and connective tissue disorders may respond to an increase in fibroblast collagenases and decreased collagen, fibronectin, and glycosaminoglycan production. Fibroblast responsiveness to tumor necrosis factor is also diminished. Potential medical uses of Pentoxifylline are reviewed.
Pentoxifylline use in dermatology
Inflamm Allergy Drug Targets 2012 Dec;11(6):422-32.PMID:22680624DOI:10.2174/187152812803590028.
Pentoxifylline is methylxanthine derivative which is used in microcirculatory disorders as a vasoactive drug. Novel immunomodulatory properties of Pentoxifylline have been reported including the down regulation of tumour necrosis factor-α synthesis and other inflammatory cytokines. Studies have shown that Pentoxifylline might be efficacious in a wide spectrum of skin diseases. This article focuses on the use of Pentoxifylline which is a safe and cheap drug in various dermatological disorders.
Pentoxifylline for alcoholic hepatitis
Cochrane Database Syst Rev 2009 Oct 7;2009(4):CD007339.PMID:19821406DOI:10.1002/14651858.CD007339.pub2.
Background: Alcoholic hepatitis is a life-threatening disease, with an average mortality of approximately 40%. There is no widely accepted, effective treatment for alcoholic hepatitis. Pentoxifylline is used to treat alcoholic hepatitis, but there has been no systematic review to assess its effects. Objectives: To assess the benefits and harms of Pentoxifylline in alcoholic hepatitis. Search strategy: The Cochrane Hepato-Biliary Group Controlled Trials Register, The Cochrane Central Register of Controlled Trials (CENTRAL) in The Cochrane Library, MEDLINE, EMBASE, Science Citation Index Expanded, LILACS, clinicaltrials.gov, and full text searches were conducted until August 2009. Manufacturers and authors were contacted. Selection criteria: All randomised clinical trials of Pentoxifylline in participants with alcoholic hepatitis compared to control were selected for inclusion. Data collection and analysis: Two authors extracted data and evaluated the risk of bias. RevMan Analysis was used for statistical analysis of dichotomous data with risk ratio (RR) and of continuous data with mean difference (MD), both with 95% confidence intervals (CI). Trial sequential analysis (TSA) was also used for statistical analysis of dichotomous and continuous data in order to control for random error. Where data were only available from one trial, we used Fisher's exact test or Student's t-test. Main results: Five trials, with a total of 336 randomised participants, were included. A total of 105 participants (31%) died. Of the five included trials, four (80%) had a high risk of bias. Meta-analysis using all five trials showed that Pentoxifylline reduced mortality compared with control (RR 0.64; 95% CI 0.46 to 0.89). However, this result was not supported by trial sequential analysis, which adjusts for multiple testing on accumulating data. Furthermore, four of the five trials were judged to have a high risk of bias, thus risking an overestimated intervention effect. Meta-analysis showed that Pentoxifylline reduced the hepatic-related mortality due to hepatorenal syndrome (RR 0.40; 95% CI 0.22 to 0.71), but trial sequential analysis did not support this result. Data from one trial suggests that Pentoxifylline may increase the occurrence of serious and non-serious adverse events compared to control. Authors' conclusions: The current available data may indicate a possible positive intervention effect of Pentoxifylline on all-cause mortality and mortality due to hepatorenal syndrome, and conversely, an increase in serious and non-serious adverse events. However, the evidence is not firm; no conclusions can be drawn regarding whether Pentoxifylline has a positive, negative, or neutral effect on participants with alcoholic hepatitis.
Pentoxifylline - a review of its use in osteoradionecrosis
Br J Oral Maxillofac Surg 2017 Apr;55(3):230-234.PMID:28034471DOI:10.1016/j.bjoms.2016.12.006.
Pentoxifylline has been used to treat complications related to fibrosis for over 20 years. Formerly used to treat those after radiotherapy such as osteoradionecrosis (ORN), it is now being tried for medication-related osteonecrosis of the jaw (MRONJ), which can occur after prolonged use of bisphosphonates. We review theories on the formation of fibrosis in patients with ORN, discuss the pharmacology of Pentoxifylline and vitamin E, and report published outcomes. To our knowledge no prospective randomised controlled trial has investigated the benefits of these agents in cases of ORN, but reported outcomes in many published case series are encouraging.
Pentoxifylline for treating venous leg ulcers
Cochrane Database Syst Rev 2012 Dec 12;12(12):CD001733.PMID:23235582DOI:10.1002/14651858.CD001733.pub3.
Background: Healing of venous leg ulcers is improved by the use of compression bandaging but some venous ulcers remain unhealed, and some people are unsuitable for compression therapy. Pentoxifylline, a drug which helps blood flow, has been used to treat venous leg ulcers. Objectives: To assess the effects of Pentoxifylline (oxpentifylline or Trental 400) for treating venous leg ulcers, compared with a placebo or other therapies, in the presence or absence of compression therapy. Search methods: For this fifth update we searched the Cochrane Wounds Group Specialised Register (searched 20 July 2012); The Cochrane Central Register of Controlled Trials (CENTRAL) (The Cochrane Library 2012, Issue 7); Ovid MEDLINE (2010 to July Week 2 2012); Ovid MEDLINE (In-Process & Other Non-Indexed Citations, July 19, 2012); Ovid EMBASE (2010 to 2012 Week 28); and EBSCO CINAHL (2010 to July 13 2012). Selection criteria: Randomised trials comparing Pentoxifylline with placebo or other therapy in the presence or absence of compression, in people with venous leg ulcers. Data collection and analysis: One review author extracted and summarised details from eligible trials using a coding sheet. One other review author independently verified data extraction. Main results: No new trials were identified for this update. We included twelve trials involving 864 participants. The quality of trials was variable. Eleven trials compared Pentoxifylline with placebo or no treatment. Pentoxifylline is more effective than placebo in terms of complete ulcer healing or significant improvement (RR 1.70, 95% CI 1.30 to 2.24). Pentoxifylline plus compression is more effective than placebo plus compression (RR 1.56, 95% CI 1.14 to 2.13). Pentoxifylline in the absence of compression appears to be more effective than placebo or no treatment (RR 2.25, 95% CI 1.49 to 3.39).More adverse effects were reported in people receiving Pentoxifylline (RR 1.56, 95% CI 1.10 to 2.22). Nearly three-quarters (72%) of the reported adverse effects were gastrointestinal. Authors' conclusions: Pentoxifylline is an effective adjunct to compression bandaging for treating venous ulcers and may be effective in the absence of compression. The majority of adverse effects were gastrointestinal disturbances.