Etofylline clofibrate
(Synonyms: 益多酯) 目录号 : GC39283
Etofylline clofibrate 具有降脂和抗血栓形成作用。Etofylline clofibrate 具有与内膜 PGI2 激动的相互作用。
Cas No.:54504-70-0
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
Etofylline clofibrate has ypolipidemic and antithrombotic effect. Etofylline clofibrate has an agonistic interaction with intimal PGI2[1].
[1]. Metz G, et al. Effect of etofylline clofibrate on experimental thrombus formation and prostacyclin activation. Arzneimittelforschung. 1986 Sep;36(9):1363-5.
| Cas No. | 54504-70-0 | SDF | |
| 别名 | 益多酯 | ||
| Canonical SMILES | ClC(C=C1)=CC=C1OC(C)(C)C(OCCN2C3=C(N(C(N(C)C3=O)=O)C)N=C2)=O | ||
| 分子式 | C19H21ClN4O5 | 分子量 | 420.85 |
| 溶解度 | DMSO: 52 mg/mL (123.56 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 | 2.3761 mL | 11.8807 mL | 23.7614 mL |
| 5 mM | 0.4752 mL | 2.3761 mL | 4.7523 mL |
| 10 mM | 0.2376 mL | 1.1881 mL | 2.3761 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 |
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| % 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。
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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.
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.
[Evaluation of the antilipaemic potential of Etofylline clofibrate, its metabolites and clofibrate in dietary-induced hyperlipidaemia in the rat (author's transl)]
Arzneimittelforschung 1980;30(11b):2038-41.PMID:7194056doi
Efficacy of 1-(theophyllin-7-yl)-ethyl-2-[2-(p-chlorophenoxy)-2-methylpropionate] (Etofylline clofibrate, ML 1024, Duolip) and its molecule components (metabolites) of structurally similar theophylline esters and of clofibrate as standard was investigated in the artificial hyperlipidaemia of the rat. In accordance with former results Etofylline clofibrate was antilipaemically active and, in contrast to similar esters and clofibrate, significantly decreased the cholesterol level. An investigation of the efficacy of its metabolites, either alone or in equivalent mixture, as well as of the standard clofibrate under fat diet demonstrated low efficacy of etofylline, but an increased activity in combination with clofibrate or clofibric acid. The activity of the combination is significantly superior to that of clofibrate under fat diet, but not under normal diet. The increased efficacy of Etofylline clofibrate is undoubtedly an unusual potentiation, an additive effect of the metabolites can be excluded. Cholesterol and triglycerides are relevant parameters for the experimental evaluation of the efficacy. Measurement of total lipids offers no additional information. Substitution of triglycerides by total-beta-lipoproteins as parameter seems methodically useful, since values of cholesterol, triglycerides and beta-lipoproteins correlate well under normal diet.
[Effect of Etofylline clofibrate on the composition of lipoproteins in hyperlipidaemia type IIb and IV (author's transl)]
Arzneimittelforschung 1980;30(11b):2063-7.PMID:7194061doi
Efficacy of 1-(theophyllin-7-yl)-ethyl-2[2-(p-chlorophenoxy)-2-methylpropionate] (Etofylline clofibrate, Duolip) (3 x 250 mg) was evaluated in a double-blind cross-over study in 20 patients of type 11b (10 and type IV (10) in comparison to a commercial drug combination (= standard preparation) of clofibrate (3 x 500 mg) and beta-pyridylcarbinol hydrogentartrate (3 x 25 mg). This standard preparation was known from clinical results to be superior over clofibrate in antilipaemic potency. All patients had been already on a diet for several months and in majority were additionally treated with antihyperlipaemic drugs. The treatment periods lasted over 8 weeks each. They were introduced by placebo phases of 4 weeks duration. Between the treatment periods with Etofylline clofibrate and with the standard preparation, placebo phases of 4 weeks were inserted, too. The results indicate, that between Etofylline clofibrate and the standard preparation there are no remarkable differences and thus 750 mg Etofylline clofibrate correspond to 1500 mg clofibrate combined with 75 mg beta-pyridylcarbinol hydrogentartrate in their efficiencies. Since the clofibric acid proportion of Etofylline clofibrate clinically is known as ineffective we postulate a potentiation of its effect by its metabolits to cause this surprising effect. In type IIb the cholesterol was distinctly decreased in the VLDL-fraction by 22% and significantly increased in the HDL-fraction by 22%. In type IV triglycerides and cholesterol dropped in the VLDL by 11% and 16%, resp., unless the LDL-fraction revealed an increase of the lipid content. The lipids of the HDL-fraction did not show any essential alternations. Side effects were not observed. The investigations prove that Etofylline clofibrate is suitable for the treatment of hyperlipoproteinaemia with elevated triglycerides and cholesterol.
Effect of Etofylline clofibrate on experimental thrombus formation and prostacyclin activation
Arzneimittelforschung 1986 Sep;36(9):1363-5.PMID:3539125doi
1-(7-Theophyllinyl)-2-ethyl-[2-(p-chlorophenoxy)-isobutyrate] (Etofylline clofibrate, theofibrate, Duolip) was shown to possess substantial thrombus disaggregating activity in the microcirculation of the hamster cheek pouch following minor vascular damage by electrical stimulation. At 12 mg/kg p.o. the moderate effect of a single dose (12% reduction in disaggregation time) increased to a maximum reduction of 31 and 43% following 5 and 7 consecutive daily applications, respectively. Etofylline clofibrate was more active than other drugs already tested in this test system, but less than the prostaglandins PGE1 and PGI2. The antithrombotic efficacy found in both in vivo tests, thrombus formation and disaggregation, suggests as mode of action of Etofylline clofibrate an agonistic interaction with intimal PGI2. This could be by enhancement of its production or by a synergistic interaction with this prostanoid, rather than inhibition of thromboxane A2 synthetase.