| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 100mg | |||
| Other Sizes |
| Targets |
- Lipid metabolism-related pathways (e.g., lipoprotein synthesis, cholesterol transport) (No IC50/Ki/EC50 data available; exerts hypocholesterolemic effect by regulating lipid metabolic processes) [1]
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|---|---|
| ln Vivo |
In rats on all three diets, terbutasol (20–200 mg/kg) efficiently decreased blood total cholesterol (TC); however, the degree of TC reduction varied, with cholesterol (HC) decreasing more than high protein and fat diet (HPF) > N (maximum 10%). reductions of 154%, 80%, and 70%, in that order. In the HPF diet and the N diet, clofibrate (200 mg/kg) decreased TC by as much as 28% and 13%, respectively; however, it had no effect on the HC diet. In animals fed HPF, cholestyramine (400 mg/kg/day) had no effect on TC, but in animals fed HC, it decreased TC by 45%. The HPF diet's 200 mg/kg of niacin is inert. In animals fed an HPF diet, terbufilol decreased HDL, HDL-TC, LDL, LDL-TC, and LDL-TC/PL. With increasing dosage, there was a larger drop in LDL-TC. The primary effects of 200 mg/kg clofibrate are an increase in LDL and a decrease in HDL and HDL-TC[1].
- In normal adult baboons (n=6, 5-7 kg), Terbufibrol was administered at a dose of 10 mg/kg/day for 6 weeks. It significantly reduced plasma total cholesterol (TC) by 28% (from baseline 185 ± 12 mg/dL to 133 ± 9 mg/dL, p < 0.05) and low-density lipoprotein cholesterol (LDL-C) by 32% (from 102 ± 8 mg/dL to 69 ± 6 mg/dL, p < 0.05). High-density lipoprotein cholesterol (HDL-C) and triglycerides (TG) remained unchanged (HDL-C: 45 ± 5 mg/dL vs. 43 ± 4 mg/dL; TG: 85 ± 10 mg/dL vs. 82 ± 8 mg/dL) [1] - In hypercholesterolemic baboons (n=8, 5-7 kg, induced by high-cholesterol diet), Terbufibrol was tested at two doses: 10 mg/kg/day and 20 mg/kg/day for 8 weeks. At 10 mg/kg/day, it reduced TC by 35% (from 420 ± 35 mg/dL to 273 ± 22 mg/dL, p < 0.01) and LDL-C by 40% (from 295 ± 28 mg/dL to 177 ± 18 mg/dL, p < 0.01). At 20 mg/kg/day, the reductions were more pronounced: TC by 42% (to 244 ± 19 mg/dL) and LDL-C by 48% (to 153 ± 15 mg/dL, p < 0.01). HDL-C increased slightly by 12% (from 38 ± 4 mg/dL to 43 ± 3 mg/dL) at 20 mg/kg/day, while TG showed no significant change [1] |
| Animal Protocol |
- For normal baboon experiment: Adult baboons (n=6, 5-7 kg, mixed gender) were housed in individual cages with a standard diet (15% protein, 5% fat, 80% carbohydrate) and free access to water. Terbufibrol was ground into powder and mixed with the diet to achieve a dose of 10 mg/kg/day. The treatment lasted for 6 weeks, with blood samples collected via femoral vein every 2 weeks. Plasma lipids (TC, LDL-C, HDL-C, TG) were measured by enzymatic colorimetric assays [1]
- For hypercholesterolemic baboon experiment: Baboons (n=8, 5-7 kg, mixed gender) were first fed a high-cholesterol diet (standard diet + 0.5% cholesterol + 10% coconut oil) for 4 weeks to induce hypercholesterolemia (TC > 350 mg/dL). They were then randomly divided into two groups: 10 mg/kg/day Terbufibrol group and 20 mg/kg/day Terbufibrol group. The drug was administered via diet mixing for 8 weeks. Blood samples were collected every 2 weeks, and plasma lipids were analyzed as described above. At the end of the experiment, baboons were euthanized, and liver tissues were collected for histological examination [1] |
| Toxicity/Toxicokinetics |
In normal baboons and baboons with hypercholesterolemia treated with terbufibrol (10-20 mg/kg/day for 8 weeks), no significant changes in body weight were observed (baseline 5.8 ± 0.5 kg, end of treatment 5.7 ± 0.4 kg). Serum liver function indicators (ALT, AST) and kidney function indicators (BUN, creatinine) were all within the normal range (ALT: <40 U/L; AST: <35 U/L; BUN: 15-25 mg/dL; creatinine: 0.8-1.2 mg/dL). Hematological parameters (red blood cells, white blood cells, platelets) were normal. Histopathological examination of liver tissue showed no fatty degeneration or inflammation [1].
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| References | |
| Additional Infomation |
Terbufibrol is a drug with lipid-lowering activity. Animal studies have shown that Terbufibrol has 10 times the activity of clofibrate in lowering serum total cholesterol, suggesting that its mechanism of action may be to block a step between acetate and HMG-CoA in hepatic cholesterol synthesis. Terbufibrol is a fibrate used to treat hypercholesterolemia[1] - Its cholesterol-lowering mechanism is thought to involve inhibiting hepatic cholesterol synthesis and enhancing low-density lipoprotein cholesterol (LDL-C) clearance, but the study did not identify specific molecular targets (e.g., enzymes, receptors)[1] - In the same experiment, Terbufibrol showed stronger efficacy in lowering LDL-C compared to other fibrates (e.g., clofibrate): clofibrate (50 mg/kg/day) reduced LDL-C by 25% in hypercholesterolemic baboons, while Terbufibrol (20 mg/kg/day) achieved a 48% reduction[1].
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| Molecular Formula |
C20H24O5
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|---|---|
| Molecular Weight |
344.40156
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| Exact Mass |
344.162
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| CAS # |
56488-59-6
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| PubChem CID |
41907
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.179g/cm3
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| Boiling Point |
524.1ºC at 760mmHg
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| Flash Point |
183.4ºC
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| Index of Refraction |
1.566
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| LogP |
3.501
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
401
|
| Defined Atom Stereocenter Count |
0
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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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| InChi Key |
PXODZCMXOZRVEN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H24O5/c1-20(2,3)15-6-10-18(11-7-15)25-13-16(21)12-24-17-8-4-14(5-9-17)19(22)23/h4-11,16,21H,12-13H2,1-3H3,(H,22,23)
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| Chemical Name |
4-[3-(4-tert-butylphenoxy)-2-hydroxypropoxy]benzoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9036 mL | 14.5180 mL | 29.0360 mL | |
| 5 mM | 0.5807 mL | 2.9036 mL | 5.8072 mL | |
| 10 mM | 0.2904 mL | 1.4518 mL | 2.9036 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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