Terbufibrol
Based on 1 Customer Validation
Terbufibrol is an orally active lipid-lowering agent. Terbufibrol inhibits hepatic Cholesterol 7 alpha-hydroxylase. Terbufibrol blocks a step between Acetate and HMG-CoA in the hepatic cholesterol synthesis process. Terbufibrol reduces serum total cholesterol, HDL, LDL, lipoprotein levels, and the cholesterol/phospholipid ratio, with dose- and sex-dependent changes in lipoprotein components. Terbufibrol exerts sustained cholesterol-lowering activity in baboons and rats. Terbufibrol can be used in research related to hypercholesterolemia.
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- Pureza: 98.39%
- No. CAS: 56488-59-6
- Fòrmula: C20H24O5
- Peso molecular:344.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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Cholesterol 7 alpha-hydroxylase |
Terbufibrol (20-200 mg/kg/day; p.o.; daily; 4 weeks) dose-dependently reduces serum total cholesterol and modulates lipoprotein cholesterol levels in HPF-diet induced endogenous hypercholesterolemic male baboons, with a maximum 80% serum TC reduction at 200 mg/kg/day and an ED50 of 60 mg/kg/day specific to this diet model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Papio cynocephalus (2-3 years old, 4-7 kg, equal numbers of males and females)[1]
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Dosage:12 mg/kg/day; 50 mg/kg/day; 200 mg/kg/day
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Administration:p.o.; daily; 8 weeks
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Result:Reduced serum total cholesterol by 6.7% after 8 weeks at 12 mg/kg/day.
Decreased VLDL by a mean of 20% and HDL by a mean of 21% respectively at 12 mg/kg/day.
Increased LDL in males by 36% at 12 mg/kg/day.
Reduced serum total cholesterol by 21.1% after 8 weeks at 50 mg/kg/day.
Decreased VLDL by a mean of 12% and HDL by a mean of 43% at 50 mg/kg/day.
Decreased LDL in males by 35% at 50 mg/kg/day.
Reduced serum total cholesterol by 69.1% after 8 weeks at 200 mg/kg/day.
Reduced total lipoprotein by a mean of 52% across sexes at 200 mg/kg/day.
Decreased LDL by a mean of 46% and HDL by a mean of 57% at 200 mg/kg/day.
Reduced LDL-TC and HDL-TC, with a greater effect on LDL-TC, increasing the HDL-TC/LDL-TC ratio by 56% compared to control at 200 mg/kg/day.
Caused a dose-related decrease in the TC/PL ratio in VLDL due to increased PL content.
Caused a dose-related decrease in the TC/PL ratio in LDL due to reduced TC content and increased TG content.
Caused a trend of decreased PL with increasing dose in HDL.
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Animal Model:Papio cynocephalus (2-3 years old, 4-7 kg, male only)[1]
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Dosage:20 mg/kg/day; 60 mg/kg/day; 200 mg/kg/day
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Administration:p.o.; daily; 4 weeks
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Result:Primarily decreased HDL-TC, reducing the HDL-TC/LDL-TC ratio by 17% at 20 mg/kg/day.
Decreased LDL-TC more than HDL-TC, increasing the HDL-TC/LDL-TC ratio from a control value of 1.8 to 4.4 (a 144% increase) at 60 mg/kg/day.
Produced a maximum 80% reduction in serum TC at 200 mg/kg/day.
Decreased LDL-TC more than HDL-TC, and also reduced HDL, HDL-TC, LDL, and LDL-TC/PL at 200 mg/kg/day.
Was approximately 10 times more active than clofibrate at reducing serum TC in this model.
Had an ED50 for serum TC reduction of 60 mg/kg/day for the HPF-diet.
Chemical Information
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No. CAS 56488-59-6
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Appearance Solid
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Peso molecular 344.40
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Fòrmula C20H24O5
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Color White to off-white
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SMILES
O=C(O)C1=CC=C(OCC(O)COC2=CC=C(C(C)(C)C)C=C2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 200 mg/mL (580.72 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (14.52 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (14.52 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[2]. Löser R, et al. Mode of action of terbufibrol (INN) a hypolipidemic agent on rat liver sterol synthesis. Artery. 1982;10(3):180-92. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9036 mL | 14.5180 mL | 29.0360 mL | 72.5900 mL |
| 5 mM | 0.5807 mL | 2.9036 mL | 5.8072 mL | 14.5180 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9036 mL | 7.2590 mL | |
| 15 mM | 0.1936 mL | 0.9679 mL | 1.9357 mL | 4.8393 mL | |
| 20 mM | 0.1452 mL | 0.7259 mL | 1.4518 mL | 3.6295 mL | |
| 25 mM | 0.1161 mL | 0.5807 mL | 1.1614 mL | 2.9036 mL | |
| 30 mM | 0.0968 mL | 0.4839 mL | 0.9679 mL | 2.4197 mL | |
| 40 mM | 0.0726 mL | 0.3630 mL | 0.7259 mL | 1.8148 mL | |
| 50 mM | 0.0581 mL | 0.2904 mL | 0.5807 mL | 1.4518 mL | |
| 60 mM | 0.0484 mL | 0.2420 mL | 0.4839 mL | 1.2098 mL | |
| 80 mM | 0.0363 mL | 0.1815 mL | 0.3630 mL | 0.9074 mL | |
| 100 mM | 0.0290 mL | 0.1452 mL | 0.2904 mL | 0.7259 mL |
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