Pentoxifylline (BL-191)
(Synonyms: 己酮可可碱) 目录号 : GC32444
An anti-inflammatory methylxanthine derivative
Cas No.:6493-05-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
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- SDS (Safety Data Sheet)
- Datasheet
Pentoxifylline is a methylxanthine derivative. It has been shown to have anti-inflammatory activity, inhibiting LPS-induced TNF-α production in isolated peripheral blood mononuclear cells (IC50 = 85 ?M) and suppressing LPS-induced leukopenia in mice.1 Pentoxifylline weakly inhibits the generation of phosphatidic acid (IC50 = 500 ?M) from LPS-activated lysophosphatidic acyl transferase (LPAAT), and weakly antagonizes A1 and A2 adenosine receptors.2,3 It also inhibits human acidic mammalian chitinase, human chitotriosidase, and chitinase B1 from Aspergillus fumigatus (IC50s = 49, 98, and 126 ?M, respectively).4
1.Cottam, H.B., Shih, H., Tehrani, L.R., et al.Substituted xanthines, pteridinediones, and related compounds as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor αJ. Med. Chem.392-9(1996) 2.Rice, G.C., Brown, P.A., Nelson, R.J., et al.Protection from endotoxic shock in mice by pharmacologic inhibition of phosphatidic acidProc. Natl. Acad. Sci. USA91(9)3857-3861(1994) 3.Schwabe, U., Ukena, D., and Lohse, M.J.Xanthine derivatives as antagonists at A1 and A2 adenosine receptorsNaunyn Schmiedebergs Arch. Pharmacol.330(3)212-221(1985) 4.Rao, F.V., Andersen, O.A., Vora, K.A., et al.Methylxanthine drugs are chitinase inhibitors: Investigation of inhibition and binding modesChem. Biol.12(9)973-980(2005)
| Cas No. | 6493-05-6 | SDF | |
| 别名 | 己酮可可碱 | ||
| Canonical SMILES | O=C(N1CCCCC(C)=O)N(C)C2=C(N(C)C=N2)C1=O | ||
| 分子式 | C13H18N4O3 | 分子量 | 278.31 |
| 溶解度 | Water : 93.3 mg/mL (335.24 mM);DMSO : ≥ 2.8 mg/mL (10.06 mM) | 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 | 3.5931 mL | 17.9656 mL | 35.9312 mL |
| 5 mM | 0.7186 mL | 3.5931 mL | 7.1862 mL |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5931 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 | ||||||||||
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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 (BL 191) by oral administration in the treatment of asthenozoospermia
Andrologia 1980 May-Jun;12(3):228-31.PMID:7004272DOI:10.1111/j.1439-0272.1980.tb00617.x.
The aim of this trial was to study the effects on semen of Pentoxifylline administered chronically per os to patients with normogonadotropic asthenozoospermia. Fifteen infertile men (age 22 to 44 years) were incorporated. Each subject was submitted to a treatment with Pentoxifylline per os at a dose of 1,200 mg per day during no less than four months (x plus or minus SE 6.6 plus or minus 0.7 months). Assessment of the results was performed by serial spermatograms performed during and up to three months after treatment. The results showed a significant improvement of the percentages of forwardly progressive spermatozoa and of live and motile spermatozoa. Five of the patients achieved a normalization of semen (frank improvement) and seven a significant improvement in comparison to the initial values. Pregnancy was obtained by two patients. Pentoxifylline could be a useful alternative for the treatment of patients with normogonadotropic asthenozoospermia.
Pharmacologic Treatment of Idiopathic Chilblains (Pernio): A Systematic Review
J Cutan Med Surg 2021 Sep;25(5):530-542.PMID:33653127DOI:10.1177/1203475421995130.
Idiopathic chilblains is a cold-induced inflammatory condition that causes significant morbidity. When preventative measures alone are inadequate, oral nifedipine is generally recommended as first-line pharmacologic therapy. Given the natural course of this spontaneously remitting/relapsing condition, controls are needed to critically appraise studies and determine the value of treatments. We report a systematic review of placebo-controlled or comparative therapeutic trials for the treatment of idiopathic chilblains. Our search of PubMed, Embase, and Cochrane databases, identified 11 studies that met our inclusion criteria for a combined study population n = 576. Therapies included nifedipine, Pentoxifylline, tadalafil, topical glyceryl trinitrate (GTN), topical minoxidil, diltiazem, corticosteroids, and vitamin D. There was moderate evidence to support the use of nifedipine and Pentoxifylline in the treatment of severe or refractory cases of idiopathic chilblains, while other therapies had inadequate evidence or nonsignificant results compared to placebo.
Pentoxifylline as a therapeutic option for pre-eclampsia: a study on its placental effects
Br J Pharmacol 2022 Nov;179(22):5074-5088.PMID:35861684DOI:10.1111/bph.15931.
Background and purpose: Recently Pentoxifylline, a non-selective phosphodiesterase inhibitor and adenosine receptor antagonist, has attracted much interest for the treatment of the increased vascular resistance and endothelial dysfunction in pre-eclampsia. We therefore investigated the placental transfer, vascular effects and anti-inflammatory actions of Pentoxifylline in healthy and pre-eclamptic human placentas. Experimental approach: The placental transfer and metabolism of Pentoxifylline were studied using ex vivo placenta perfusion experiments. In wire myography experiments with chorionic plate arteries, pentoxifyllines vasodilator properties were investigated, focusing on the cGMP and cAMP pathways and adenosine receptors. Its effects on inflammatory factors were also studied in placental explants. Key results: Pentoxifylline transferred from the maternal to foetal circulation, reaching identical concentrations. The placenta metabolized Pentoxifylline into its active metabolite lisofylline (M1), which was released into both circulations. In healthy placentas, Pentoxifylline potentiated cAMP- and cGMP-induced vasodilation, as well as causing vasodilation by adenosine A1 antagonism and via NO synthase and PKG. Pentoxifylline also reduced inflammatory factors secretion. In pre-eclamptic placentas, we observed that its vasodilator capacity was preserved, however not via NO-PKG but likely through adenosine signalling. Pentoxifylline neither potentiated vasodilation through cAMP and cGMP, nor suppressed the release of inflammatory factors from these placentas. Conclusion and implications: Pentoxifylline is transferred across and metabolized by the placenta. Its beneficial effects on the NO pathway and inflammation are not retained in pre-eclampsia, limiting its application in this disease, although it could be useful for other placenta-related disorders. Future studies might focus on selective A1 receptor antagonists as a new treatment for pre-eclampsia.
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-伪 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.