Etofylline
(Synonyms: 乙羟茶碱; 7-(β-Hydroxyethyl)theophylline) 目录号 : GC34037
A PDE inhibitor
Cas No.:519-37-9
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
7-(β-Hydroxyethyl)theophylline is a methylxanthine phosphodiesterase (PDE) inhibitor.1 It reduces histamine, 5-hydroxytryptamine, and bradykinin-induced bronchoconstriction in an anesthetized guinea pig model of bronchial asthma.2 Formulations containing 7-(β-hydroxyethyl)theophylline in combination with theophylline have been used in the treatment of asthma.
1.Mizon, J., Skandrani, E., and Mizon, C.Determination of the inhibitory activity of some new substituted theophyllines on the specific phosphodiesterase of cyclic nucleotidesTherapie26(5)911-917(1971) 2.Ufkes, J.G., Leeuwin, R.S., Ottenhof, M., et al.Efficacy of theophylline and its N-7-substituted derivatives in experimentally induced bronchial asthma in the guinea-pigArch. Int. Pharmacodyn. Ther.253(2)301-314(1981)
| Cas No. | 519-37-9 | SDF | |
| 别名 | 乙羟茶碱; 7-(β-Hydroxyethyl)theophylline | ||
| Canonical SMILES | O=C(N1C)N(C)C2=C(N(CCO)C=N2)C1=O | ||
| 分子式 | C9H12N4O3 | 分子量 | 224.22 |
| 溶解度 | DMSO : ≥ 100 mg/mL (445.99 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 | 4.4599 mL | 22.2995 mL | 44.5991 mL |
| 5 mM | 0.892 mL | 4.4599 mL | 8.9198 mL |
| 10 mM | 0.446 mL | 2.23 mL | 4.4599 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。
Mannose-anchored N,N,N-trimethyl chitosan nanoparticles for pulmonary administration of Etofylline
Int J Biol Macromol 2020 Dec 15;165(Pt A):445-459.PMID:32987078DOI:10.1016/j.ijbiomac.2020.09.163.
Drug delivery to lungs via pulmonary administration offers potential for the development of new drug delivery systems. Here we fabricated the Etofylline (ETO) encapsulated mannose-anchored N,N,N-trimethyl chitosan nanoparticles (Mn-TMC NPs). The prominent characteristics like biocompatibility, controlled release, targeted delivery, high penetrability, enhanced physical stability, and scalability mark Mn-TMC NPs as a viable alternative to various nanoplatform technologies for effective drug delivery. Mannosylation of TMC NPs leads to the evolution of new drug delivery vehicle with gratifying characteristics, and potential benefits in efficient drug therapy. It is widely accepted that following pulmonary administration, the introduction of mannose to the surface of drug nanocarriers provide selective macrophage targeting via receptor-mediated endocytosis. The fabricated Mn-TMC NPs exhibited particle size of 223.3 nm, PDI 0.490, and ζ-potential -19.1 mV, drug-loading capacity 76.26 ± 1.2%, and encapsulation efficiency of 91.75 ± 0.88%. Sustained drug release, biodegradation studies, stability, safety, and aerodynamic behavior revealed the effectiveness of prepared nanoformulation for pulmonary administration. In addition, the in vivo pharmacokinetic studies in Wistar rat model revealed a significant improvement in therapeutic efficacy of ETO, illustrating mannosylation a promising approach for efficient therapy of airway diseases following pulmonary administration.
Pharmacokinetics of Etofylline after intravenous and oral administration to humans
Int J Clin Pharmacol Ther Toxicol 1981 Jul;19(7):310-3.PMID:7263108doi
Etofylline is used in many countries as a bronchodilator. In a cross-over study in healthy volunteers serum concentrations and urinary excretion were studied after administration of Etofylline (= beta-hydroxyethyltheophylline), intravenously and orally at a dose of 200 mg. Etofylline is a N-7 substituted theophylline derivative which dose not release theophylline in vitro or in vivo. It therefore has its own pharmacokinetic and pharmacodynamic properties. Its plasma decay after intravenous administration shows two-compartment kinetics with a rapid distribution. The alpha-phase lasted on the average 20 min and beta was 0.175 h(-1), corresponding with a beta-phase half-life of 4.1 h. The mean volume of distribution was 0.60 liter/kg, total body clearance 0.106 l.kg(-1).h(-1), and the renal clearance about 0.017 l.kg(-1).h(-1). About 20% of the drug is excreted unchanged in the urine. The curve determined after oral administration can be described by one-compartment kinetics. A comparison of the areas under the curve suggests that the drug was rapidly but incompletely absorbed from the gastrointestinal tract. Its bioavailability was about 80%. Mean peak levels of Etofylline were about 3.9 mg/liter after oral administration. The normal dose advocated is 50-100 mg three times a day. With the Wagner-Nelson equation a mean steady state level for this dose can be calculated at about 0.7-1.4 g/ml. Since no information is available on the pharmacodynamic properties, no conclusion can be drawn about the therapeutic effectiveness of the drug.
Teratological study of the hypolipidaemic drugs Etofylline clofibrate (VULM) and fenofibrate in Swiss mice
Pharmacol Toxicol 1989 Mar;64(3):286-90.PMID:2726692DOI:10.1111/j.1600-0773.1989.tb00648.x.
Teratological studies of the hypolipidaemic drugs Etofylline clofibrate (VULM) and fenofibrate were carried out in mice. Pregnant mice were given Etofylline clofibrate and fenofibrate in doses 11.7, 117.1, and 585.5 mg/kg orally from day 7 to 16 of gestation. Terminal maternal body weight was significantly decreased after all doses of Etofylline clofibrate in a non-dose-related fashion compared to the control group. The foetuses were examined on day 19 of gestation. They were weighed and inspected for external, skeletal and visceral abnormalities. The low and middle doses of Etofylline clofibrate and fenofibrate had no adverse effects on embryofoetal development. The highest Etofylline clofibrate dose induced a significant decrease of foetal weight at term, likewise postimplantation loss was significantly increased after the highest dose of fenofibrate. The incidence of external, skeletal and visceral anomalies was not dose-dependent. In this study no teratogenic effects were detected, yet with the highest Etofylline clofibrate and fenofibrate doses some foetotoxic effects were observed.
A simple and rapid HPLC/UV method for the simultaneous quantification of theophylline and Etofylline in human plasma
J Chromatogr B Analyt Technol Biomed Life Sci 2007 Apr 1;848(2):271-6.PMID:17110179DOI:10.1016/j.jchromb.2006.10.035.
A simple, sensitive and selective high performance liquid chromatography (HPLC) method with ultraviolet detection (272 nm) was developed and validated for the simultaneous quantification of theophylline and Etofylline in human plasma. Following rapid sample preparation, the analytes and internal standard (hydrochlorothiazide) were separated using an isocratic mobile phase on a reverse phase C18 column. The lower limit of quantification was 100 ng/mL for both theophylline and Etofylline with a relative standard deviation of less than 6%. A linear dynamic range of 100-10,000 ng/mL for both theophylline and Etofylline was established. This HPLC method was validated with between-batch precision of 2.2-6.0 and 1.4-3.7% for theophylline and Etofylline, respectively. The between-batch accuracy was 94.3-98.0 and 95.4-98.2%, respectively. Stability of theophylline and Etofylline in plasma was excellent, with no evidence of degradation during sample processing (autosampler) and 30 days storage in a freezer. This validated method is simple and rugged enough to be used in pharmacokinetic studies.
Effect of Etofylline clofibrate on experimental thrombosis and platelet function
Arzneimittelforschung 1980;30(11b):2042-5.PMID:7194057doi
1-(Theophyllin-7yl)-ethyl-2-[2-(p-chlorophenoxy)-2-methylpropionate] (Etofylline clofibrate, ML 1024, Duolip) was shown to be a potent inhibitor of experimental thrombus formation in the microvasculature of the hamster cheek pouch and of platelet aggregation and adhesiveness in the cynomolgus monkey. Inhibitory effect on thrombus formation was superior to that obtained with either of the molecule components (clofibric acid and Etofylline) or their 1 : 1 mixture and a synergistic effect was apparent. Etofylline clofibrate was more active than a commercial antithrombotic drug combination of acetylsalicylic acid (ASA) and dipyridamole as an inhibitor of thrombus formation in this test system (p less than 0.05) at the proposed therapeutic dose level for each drug. In the cynomolgus monkey, Etofylline clofibrate was shown again to be a potent inhibitor of platelet aggregation induced by ADP and collagen and of platelet adesiveness after administration of 12 mg/kg/day for 21 days. A mixture of clofibrate and Etofylline (21.25 mg/kg/day and 3.75 mg/kg/day, respectively) had relatively less effect on platelet aggregation and no consistent effect on platelet adhesiveness. The activity found in both test systems indicates a promising antithrombotic potential for Etofylline clofibrate and warrants further investigation in humans.