| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Other Sizes |
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorption from the gastrointestinal tract is limited and variable (about 7%). Biological Half-Life Ranges from 12 hours to more than 500 hours, the longest half-life probably being in adipose tissue. |
|---|---|
| References | |
| Additional Infomation |
Probucol is a dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood. It has a role as an anticholesteremic drug, an antioxidant, an anti-inflammatory drug, a cardiovascular drug and an antilipemic drug. It is a dithioketal and a polyphenol.
A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993). Probucol has been reported in Penicillium citrinum with data available. Probucol is a bis-phenol antioxidant with antilipidemic activity. Probucol inhibits oxidation of low density lipoprotein and lowers the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism. A drug used to lower LDL and HDL cholesterol yet has little effect on serum-triglyceride or VLDL cholesterol. (From Martindale, The Extra Pharmacopoeia, 30th ed, p993). Drug Indication Used to lower LDL and HDL cholesterol. Mechanism of Action Probucol lowers serum cholesterol by increasing the fractional rate of low-density lipoprotein (LDL) catabolism in the final metabolic pathway for cholesterol elimination from the body. This drug may also act to inhibit the initial stages of cholesterol synthesis and act to inhibit the absorption of cholesterol from the diet. Recent information suggests that probucol may inhibit the oxidation and tissue deposition of LDL cholesterol, thereby inhibiting atherogenesis. It appears to inhibits ABCA1-mediated cellular lipid efflux. Pharmacodynamics Probucol lowers cholesterol levels by increasing LDL (low-density lipoprotein) breakdown. Additionally, probucol may inhibit cholesterol synthesis and delay cholesterol absorption. Probucol is a powerful antioxidant drug normally used to prevent vascular disease caused by the free radicals in the body. |
| Exact Mass |
516.309
|
|---|---|
| CAS # |
23288-49-5
|
| Related CAS # |
Probucol (Standard);23288-49-5;Probucol-13C3;1173019-29-8;Probucol-d6
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| PubChem CID |
4912
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
546.7±50.0 °C at 760 mmHg
|
| Melting Point |
117 118ºC
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| Flash Point |
264.9±28.8 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
|
| Index of Refraction |
1.574
|
| LogP |
10.27
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
|
| Heavy Atom Count |
35
|
| Complexity |
583
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
S(C(C([H])([H])[H])(C([H])([H])[H])SC1C([H])=C(C(=C(C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])O[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])C1C([H])=C(C(=C(C=1[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])O[H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H]
|
| InChi Key |
FYPMFJGVHOHGLL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C31H48O2S2/c1-27(2,3)21-15-19(16-22(25(21)32)28(4,5)6)34-31(13,14)35-20-17-23(29(7,8)9)26(33)24(18-20)30(10,11)12/h15-18,32-33H,1-14H3
|
| Chemical Name |
2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulfanylpropan-2-ylsulfanyl]phenol
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| Synonyms |
Probucol Biphenabid Lorelco
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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) |
DMSO : ≥ 100 mg/mL (~193.48 mM)
H2O : ~0.67 mg/mL (~1.30 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.84 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01000467 | COMPLETED | Drug: probucol Drug: probucol Drug: probucol |
Healthy | Korea Otsuka Pharmaceutical Co., Ltd | 2009-02 | Phase 4 |
| NCT06225752 | NOT YET RECRUITING | Drug: Probucol Drug: Placebo probucol |
Ischemic Stroke TIA |
First Affiliated Hospital of Wannan Medical College |
2024-04-01 | Phase 3 |
| NCT01590901 | COMPLETED | Drug: Probucol | Healthy | Otsuka Beijing Research Institute | 2012-02 | Phase 1 |
| NCT02707458 | COMPLETED | Drug: Probucol | Age-related Cognitive Decline Dementia of the Alzheimer Type Mild Cognitive Impairment Due to Alzheimer Disease |
Douglas Mental Health University Institute | 2016-04 | Phase 1 Phase 2 |
| NCT01252056 | COMPLETED | Drug: Probucol Drug: Probucol and Cilostazol |
Diabetic Nephropathy | Otsuka Beijing Research Institute | 2010-03 | Phase 4 |
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