Absorption, Distribution and Excretion
Absorption in the gastrointestinal tract is limited and variable (approximately 7%). Biological Half-Life Ranges from 12 hours to over 500 hours, with the longest half-life likely occurring in adipose tissue.

[1]. Probucol.

Probucol is a dithioacetate with the structure propane-2,2-dithiol, in which the hydrogen atoms connecting the two sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl. It is a cholesterol-lowering drug with antioxidant and anti-inflammatory properties, used to treat hypercholesterolemia. Probucol has multiple effects, including cholesterol-lowering, antioxidant, anti-inflammatory, cardiovascular disease, and lipid-lowering. It is a dithioacetate and polyphenol compound. Probucol is used to lower low-density lipoprotein cholesterol (LDL) and high-density lipoprotein cholesterol (HDL), but has little effect on serum triglycerides or very low-density lipoprotein cholesterol (VLDL). (From Martindale Pharmacopoeia, 30th edition, p. 993). Probucol has been reported to be found in Penicillium citrinum, and relevant data exist. Probucol is a bisphenol antioxidant with lipid-lowering activity. Probucol lowers blood cholesterol levels by increasing the catabolism rate of low-density lipoprotein (LDL) and inhibiting LDL oxidation. This drug is used to lower LDL and HDL cholesterol, but has little effect on serum triglycerides or very low-density lipoprotein (VLDL) cholesterol. (Excerpt from Martindale Pharmacopoeia, 30th edition, p. 993). Drug Indications: For lowering LDL and HDL cholesterol. Mechanism of Action: Probucol lowers serum cholesterol by increasing the catabolism rate of low-density lipoprotein (LDL) in the final pathway of cholesterol metabolism. This drug may also inhibit the initial stages of cholesterol synthesis and 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 the development of atherosclerosis. It appears to inhibit ABCA1-mediated cellular lipid efflux.

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Pharmacodynamics
Probucol lowers cholesterol levels by increasing the breakdown of low-density lipoprotein (LDL). In addition, probucol may inhibit cholesterol synthesis and slow cholesterol absorption. Probucol is a potent antioxidant commonly used to prevent vascular diseases caused by free radicals in the body.

516.309

23288-49-5

Probucol (Standard);23288-49-5;Probucol-13C3;1173019-29-8;Probucol-d6

4912

White to off-white solid powder

1.1±0.1 g/cm3

546.7±50.0 °C at 760 mmHg

117 118ºC

264.9±28.8 °C

0.0±1.5 mmHg at 25°C

1.574

10.27

2

4

8

35

583

0

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]

FYPMFJGVHOHGLL-UHFFFAOYSA-N

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

2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulfanylpropan-2-ylsulfanyl]phenol

Probucol Biphenabid Lorelco

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ≥ 100 mg/mL (~193.48 mM)
H2O : ~0.67 mg/mL (~1.30 mM)

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.

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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.

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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.
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 corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)