TA-7552
(Synonyms: 二甲基4-(3,4-二甲氧苯基)-1-羟基-5,6,7-三甲氧基萘-2,3-二甲酸基酯) 目录号 : GC32609
TA-7552是一种有效的胆固醇降低剂。
Cas No.:104756-72-1
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
Animal experiment: | Male Sprague-Dawley rats (4 weeks of age) are used in this experiment. In the mechanism study, rats are divided into two or three groups of 4 to 6 animals so that the mean body weight, which varies from 210 g to 330 g, is similar between the groups. The experimental groups are treated with TA-7552 (0.1% in CE-2 powder) or cholestyramine (5% in CE-2 powder) by feeding the diet ad libitum for a period of time; The control groups are fed CE-2 powder. When the feces are collected, the animals are individually housed in a metabolic cage, and the collected feces are lyophylized and stored at -20°C[1]. |
References: [1]. Takashima K, et al. The hypocholesterolemic action of TA-7552 and its effects on cholesterol metabolism in the rat. Atherosclerosis. 1994 Jun;107(2):247-57. | |
TA-7552 is a potent cholesterol-lowering agent.
TA-7552 is a potent cholesterol-lowering agent. When TA-7552 is mixed with unsupplemented CLEA CE-2 powder in a concentration of 0.05% and administered to rats for 7 days, TA-7552 does not reduce the normal level of serum cholesterol. The hypocholesterolemic effect of TA-7552 is apparent at the lowest concentration (0.01%) of the drug in the diet, corresponding to a daily dose of ~10 mg/kg body weight, and maximal at the highest concentration of 0.2% TA-7552, lowering serum total cholesterol by 72% while elevating serum HDL cholesterol by 88%. TA-7552 also dose dependently suppresses this rise of hepatic cholesterol, and its lowering rate at the maximal dose is 90%[1].
[1]. Takashima K, et al. The hypocholesterolemic action of TA-7552 and its effects on cholesterol metabolism in the rat. Atherosclerosis. 1994 Jun;107(2):247-57.
| Cas No. | 104756-72-1 | SDF | |
| 别名 | 二甲基4-(3,4-二甲氧苯基)-1-羟基-5,6,7-三甲氧基萘-2,3-二甲酸基酯 | ||
| Canonical SMILES | O=C(C1=C(C(OC)=O)C(C2=CC=C(OC)C(OC)=C2)=C3C(OC)=C(OC)C(OC)=CC3=C1O)OC | ||
| 分子式 | C25H26O10 | 分子量 | 486.47 |
| 溶解度 | Soluble in DMSO | 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 | 2.0556 mL | 10.2781 mL | 20.5563 mL |
| 5 mM | 0.4111 mL | 2.0556 mL | 4.1113 mL |
| 10 mM | 0.2056 mL | 1.0278 mL | 2.0556 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。
The hypocholesterolemic action of TA-7552 and its effects on cholesterol metabolism in the rat
Atherosclerosis 1994 Jun;107(2):247-57.PMID:7980699DOI:10.1016/0021-9150(94)90026-4.
The hypocholesterolemic property of 1-(3,4-dimethoxyphenyl)-2,3- bis(methoxycarbonyl)-4-hydroxy-6,7,8-trimethoxynaphthalene (TA-7552) and its effects on cholesterol metabolism were investigated in the rat. TA-7552 incorporated into a hypercholesterolemic diet at a concentration of 0.2% and administered for 7 days reduced serum cholesterol by 72% and liver cholesterol by 90%, and its minimal effective dose was 0.01% in the diet. Its hypocholesterolemic effect was associated with an elevation of serum HDL-cholesterol. Inclusion of 0.1% TA-7552 in the normal laboratory chow accelerated fecal excretion of 14C derived from orally administered 4-[14C]cholesterol or carbonyl-[14C]taurocholate. The net amounts of fecal neutral sterols and bile acids were markedly increased by the same treatment. Hepatic bile acid production and hepatic and intestinal cholesterol biosynthesis as measured by cholesterol 7 alpha-hydroxylase activity and 1-[14C]acetate incorporation into tissue cholesterol, respectively, were both stimulated by the drug treatment. All these data indicate that this hypocholesterolemic agent inhibits intestinal absorption of both cholesterol and bile acids and compensatorily stimulates hepatic production of bile acids and cholesterol.
Enhancement of oral bioavailability and pharmacological effect of 1-(3,4-dimethoxyphenyl)-2,3-bis(methoxycarbonyl)-4-hydroxy-6,7,8- trimethoxynaphthalene (TA-7552), a new hypocholesterolemic agent, by micronization in co-ground mixture with D-mannitol
Biol Pharm Bull 1996 May;19(5):741-7.PMID:8741587DOI:10.1248/bpb.19.741.
To improve the bioavailability of the sparingly water-soluble drug, 1-(3,4-dimethoxyphenyl)-2,3-bis(methoxycarbonyl)-4-hydroxy-6,7,8- trimethoxynaphthalene (TA-7552), the usefulness of the co-grinding method with D-mannitol was investigated. The co-grinding was performed at various weight ratios of TA-7552 and D-mannitol using a ball mill. The particle size was markedly reduced with increasing amount of D-mannitol. A mixture ratio greater than or equal to 1:3 of the drug and D-mannitol produced submicron-sized particles. In dogs, bioavailability increased with increasing amount of D-mannitol. The 1:9 co-ground mixture gave complete absorption, as did a lecithin solution of the drug. Even co-ground powders with lower amounts of D-mannitol provided relatively high bioavailability in comparison with ground drug powder alone of a similar particle size. Further, pharmacological examination using rats indicated that the inhibition of cholesterol absorption was intestified with the reduction of particle size. These findings suggest that the co-grinding method with D-mannitol is useful for enhancing the bioavailability and pharmacological effectiveness of this sparingly water-soluble drug.
Arylnaphthalene lignans as novel series of hypolipidemic agents raising high-density lipoprotein level
Chem Pharm Bull (Tokyo) 1995 Oct;43(10):1701-5.PMID:8536344DOI:10.1248/cpb.43.1701.
A series of arylnaphthalene lignans were synthesized and tested for hypolipidemic activity. The most potent compound (4b) (TA-7552) not only reduced serum cholesterol, but also increased high-density lipoproteins cholesterol in rats. The effective dose of 4b is 100 times less than that of cholestyramine. Structure-activity relationships are discussed.