2. Anti-infection Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Virus Protease Apoptosis Reactive Oxygen Species Glutathione Peroxidase Caspase
  4. Probucol

Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases.

For research use only. We do not sell to patients.

Probucol Chemical Structure

Probucol Chemical Structure

CAS No. : 23288-49-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
100 mg In-stock
500 mg In-stock
1 g   Get quote  
5 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Probucol:

Probucol Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Probucol

View All Caspase Isoform Specific Products:

View All Isoforms
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Probucol (DH-581) is an anti-hyperlipidemic agent. Probucol activates glutathione peroxidase. Probucol promotes low density lipoprotein (LDL) catabolism, inhibits ABCA1-dependent cholesterol efflux, and decreases HDL-C levels. Probucol also has anti-inflammatory, antioxidant and neuroprotective properties. Probucol can be used for researches on bone, cardiovascular, cancer, neurological, and metabolism-related diseases[1][2][3][4][5][6][7][8][9][10][11][12][13].

IC50 & Target[13]

Caspase 3

 

Caspase 9

 

Cellular Effect
Cell Line Type Value Description References
THP-1 IC50
0.6 μM
Compound: 22
Antioxidant activity in human THP1 cells assessed as inhibition of macrophage-mediated LDL oxidation after 24 hrs in presence of CuSO4 by TBARS assay
Antioxidant activity in human THP1 cells assessed as inhibition of macrophage-mediated LDL oxidation after 24 hrs in presence of CuSO4 by TBARS assay
[PMID: 30015075]
In Vitro

Probucol (10 μM, 2 h) inhibits ABCA1-mediated cholesterol efflux by affecting the ABCA1 translocation to the plasma membrane, the membrane cholesterol pool, and the 125I-apo-AI binding in J774 macrophages expressing ABCA1[3].
Probucol (10 μM, 24 h) promotes high glucose-induced proliferation and inhibits apoptosis by reducing reactive oxygen species generation in Müller cells[5].
Probucol (0.01–0.1 mL of a 50 mg probucol/mlacetone solution, 60 min) inhibits peroxidation of microsomal membrane lipids and DNA damage induced by Fe-NTA plus H2O2[6].
Probucol (3-10 μM) protects neuroblastoma cells from peroxide-induced damage by activating glutathione peroxidase (GPx)[7].
Probucol (10 μM) promotes osteoblasts differentiation of MC3TE-E1 cells through reducing oxidative stress[11].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Probucol Related Antibodies

Apoptosis Analysis[5]

Cell Line: Müller cells treated with hyperglycemia (30 mM)
Concentration: 10 μM
Incubation Time: 24 h
Result: Attenuated hyperglycemia-induced apoptosis (4% compared to 7.7%) (annexin V-FITC/PI staining).
In Vivo

Probucol (48 mg/day, diet, 12 weeks) alleviates atherosclerosis by accelerating the process of reverse cholesterol transport, improving the anti-inflammatory and anti-oxidant functions in rabbits[4].
Probucol (60 mg/kg, i.p., 2 weeks) promotes endogenous antioxidants and provides protection against adriamycin-induced cardiomyopathy in Sprague-Dawley rats[8].
Probucol (cumulative dose, 120 mg/kg, i.p., 4 weeks) provide complete protection against adriamycin cardiomyopathy without interfering with its antitumor effect in Sprague-Dawley rats[9].
Probucol (500 mg/kg, intracavernosal injection, daily) enhances the therapeutic efficiency of mesenchymal stem cells in the treatment of erectile dysfunction in diabetic SD rats by prolonging their survival time via Nrf2 pathway[10].
Probucol (1-3.5 mg/kg, p.o., 12 weeks) promotes prevents osteoporosis development through reducing oxidative stress in hormone-deficiency-induced postmenopausal osteoporosis SD rats[11].
Probucol (61 mg/kg, p.o., 80 days) exerts multiple beneficial morphological effects that result in better left ventricular remodeling and function, reduced neurohumoral activation, and preserved renal function in the rats[12].
Probucol (500-1000 mg/kg, p.o., once a day for 15 days) recovers pathological damage of myocardial tissue through improvement of myocardium-related proteins Caspase-3 and Caspase-9 in viral myocarditis rats[13].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: New Zealand white male rabbits fed a high fat diet supplemented with 1% (w/w) cholesterol, 8% lard (w/w) and 0.05% cholate (w/w)[4]
Dosage: 48 mg/rabbit/day (400 ppm, 120 g of food intake daily)
Administration: Diet, 12 weeks
Result: Improved the paraoxonase 1 activity, cholesterol efflux rates, expression of ABCA1 and SR-BI in hepatocytes and peritoneal macrophages, and the level of ABCA1 and SR-BI in aortic lesions.
Decreased the serum HDL cholesterol concentration, myeloperoxidase activity, the IMT and the percentage plaque area of aorta.
Clinical Trial
Molecular Weight

516.84

Formula

C31H48O2S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(SC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1)(SC2=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C2)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (193.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9348 mL 9.6742 mL 19.3483 mL
5 mM 0.3870 mL 1.9348 mL 3.8697 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.84 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.97%

SDS (393 KB)

COA (249 KB) HNMR (205 KB) LCMS (126 KB)

Handling Instructions (2659 KB)
References

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9348 mL 9.6742 mL 19.3483 mL 48.3709 mL
5 mM 0.3870 mL 1.9348 mL 3.8697 mL 9.6742 mL
10 mM 0.1935 mL 0.9674 mL 1.9348 mL 4.8371 mL
15 mM 0.1290 mL 0.6449 mL 1.2899 mL 3.2247 mL
20 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4185 mL
25 mM 0.0774 mL 0.3870 mL 0.7739 mL 1.9348 mL
30 mM 0.0645 mL 0.3225 mL 0.6449 mL 1.6124 mL
40 mM 0.0484 mL 0.2419 mL 0.4837 mL 1.2093 mL
50 mM 0.0387 mL 0.1935 mL 0.3870 mL 0.9674 mL
60 mM 0.0322 mL 0.1612 mL 0.3225 mL 0.8062 mL
80 mM 0.0242 mL 0.1209 mL 0.2419 mL 0.6046 mL
100 mM 0.0193 mL 0.0967 mL 0.1935 mL 0.4837 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Probucol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Probucol23288-49-5DH-581DH581DH 581Virus ProteaseApoptosisReactive Oxygen SpeciesGlutathione PeroxidaseCaspaseCholesterol effluxAtherosclerosisAnti-inflammatoryAnti-oxidantJ774Müller cellsanti-hyperlipidemicLDLCardiomyopathyHeart FailureInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Probucol
Cat. No.:
HY-B0388
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.