Terbufibrol
(Synonyms: 特丁贝罗) 目录号 : GC31457
Terbufibrol在正常和高胆固醇血症雄性大鼠中，高效降低血清总胆固醇(TC)水平。
Cas No.:56488-59-6
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
Animal experiment: | Baboon[1] Eighteen baboons (9 male, 9 female) are given the N-diet throughout, divided into 3 groups of 6 animals, and treated with Terbufibrol for 8 weeks, as follows: Group 1: control; Group 2: 50 mg/kg per day; Group 3: 200 mg/kg per day. |
References: [1]. Howard AN, et al. The hypocholesterolemic effect of terbufibrol and other drugs in normal and hypercholesterolemic baboons. Atherosclerosis. 1979 Apr;32(4):367-80. | |
Terbufibrol has been shown highly active in reducing serum total cholesterol (TC) levels in the normal and hypercholesterolemic male rat.
Terbufibrol (20-200 mg/kg) is active in lowering serum TC in animals on all 3 diets, but the extent of cholesterol reduction varies in the order cholesterol (HC)>high protein and fat diet (HPF)>N (max. reductions: 154, 80, and 70%, respectively). Clofibrate (200 mg/kg) decreases TC by a maximum of 28% with the HPF-diet and 13% with the N-diet but is inactive with the HC-diet. Cholestyramine (400 mg/kg/day) is inactive in HPF-fed animals but reduces TC in HC-fed animals by 45%. With the HPF-diet nicotinic acid (200 mg/kg) is inactive. Terbufibrol lowers HDL, HDL-TC, LDL, LDL-TC and LDL-TC/PL in animals fed HPF-diet. A greater decrease of LDL-TC occurres with increasing dose. The main effect of Clofibrate (200 mg/kg) is to reduce HDL and HDL-TC and to increase LDL[1].
[1]. Howard AN, et al. The hypocholesterolemic effect of terbufibrol and other drugs in normal and hypercholesterolemic baboons. Atherosclerosis. 1979 Apr;32(4):367-80.
| Cas No. | 56488-59-6 | SDF | |
| 别名 | 特丁贝罗 | ||
| Canonical SMILES | O=C(O)C1=CC=C(OCC(O)COC2=CC=C(C(C)(C)C)C=C2)C=C1 | ||
| 分子式 | C20H24O5 | 分子量 | 344.4 |
| 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 | 2.9036 mL | 14.518 mL | 29.036 mL |
| 5 mM | 0.5807 mL | 2.9036 mL | 5.8072 mL |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9036 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。
Mode of action of terbufibrol (INN) a hypolipidemic agent on rat liver sterol synthesis
In an in vitro assay, rat liver cholesterol synthesis from acetate (14C-labelled) was inhibited by the hypolipidemic compound Terbufibrol (6, 11). In contrast to this, Terbufibrol in the same concentration showed hardly any effect on cholesterol synthesis with HMG-CoA (3-hydroxy-3-methylglutaryl-CoA) and mevalonate as precursors. However, liver cytosols of rats pretreated with Terbufibrol (100 mg/kg), showed in vitro double cholesterol synthesis with the precursors acetate and HMG-CoA and practically no effect with mevalonate compared to controls. This stimulating effect of Terbufibrol on sterol synthesis was observed during the basal period as well as at the maximum during the diurnal rhythm of that metabolic pathway. With the help of inhibitors of protein (Cycloheximide) and RNA (Actinomycin D) synthesis it was shown that the stimulating effect of Terbufibrol on liver cholesterol synthesis was dependent on de novo protein synthesis. Further it was observed that the hepatic cholesterol 7 alpha-hydroxylase reaction was inhibited in a dose related fashion after pretreatment with Terbufibrol. From our results it was concluded that Terbufibrol blocks the hepatic cholesterol synthesis in a step between acetate and HMG-CoA.