Page last updated: 2024-12-08
succinobucol
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Description
succinobucol: monosuccinic acid ester of probucol; a metabolically stable modification of probucol, an equipotent antioxidant to probucol but is pharmacologically distinct [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 216325 |
| CHEMBL ID | 83626 |
| CHEBI ID | 177810 |
| SCHEMBL ID | 347492 |
| MeSH ID | M0497767 |
Synonyms (51)
| Synonym |
|---|
| CHEMBL83626 , |
| CHEBI:177810 |
| 4-[2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulanylpropan-2-ylsulanyl]phenoxy]-4-oxobutanoic acid |
| agz-1067 |
| agi-1067 |
| succinobucol |
| 216167-82-7 |
| succinobucol (usan) |
| D06648 |
| succinic acid mono-{2,6-di-tert-butyl-4-[1-(3,5-di-tert-butyl-4-hydroxy-phenylsulfanyl)-1-methyl-ethylsulfanyl]-phenyl} ester |
| bdbm50117525 |
| probucol monosuccinate |
| 4-[2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulfanylpropan-2-ylsulfanyl]phenoxy]-4-oxobutanoic acid |
| probucol monosuccinae |
| agi1067 |
| 4-(4-((1-((3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)sulfanyl)-1-methylethyl)sulfanyl)-2,6-bis(1,1-dimethylethyl)phenoxy)-4-oxobutanoic acid |
| butanedioic acid, mono(4-((1-((3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)thio)-1-methylethyl)thio)-2,6-bis(1,1-dimethylethyl)phenyl) ester |
| succinobucol [usan:inn] |
| unii-j1j54v24r4 |
| j1j54v24r4 , |
| agi 1067 |
| FT-0674682 |
| butanedioic acid,1-[4-[[1-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]thio]-1-methylethyl]thio]-2,6-bis(1,1-dimethylethyl)phenyl]ester |
| succinobucol [inn] |
| succinobucol [usan] |
| succinobucol [mi] |
| S6420 |
| DB05399 |
| SCHEMBL347492 |
| CS-7896 |
| 4-(2,6-di-tert-butyl-4-((2-((3,5-di-tert-butyl-4-hydroxyphenyl)thio)propan-2-yl)thio)phenoxy)-4-oxobutanoic acid |
| DTXSID10176003 |
| AKOS030254650 |
| J-014180 |
| succinobucolagi 1067) |
| HY-14937 |
| BS-16625 |
| Q27095589 |
| mfcd08690469 |
| BCP31601 |
| agi-1067; agi-1067; agi1067; probucol monosuccinate |
| nsc810340 |
| nsc-810340 |
| HMS3746A21 |
| agi-1067;probucol monosuccinate |
| SC5126 |
| agi 10674 |
| EX-A5058 |
| AC-36902 |
| 4-(2,6-di-tert-butyl-4-((2-((3,5-di-tert-butyl-4-hydroxyphenyl)thio)propan-2-yl)thio)phenoxy)-4-oxobutanoicacid |
| c35h52o5s2 |
Research Excerpts
Overview
Succinobucol is a novel derivative of probucol with improved antioxidant and anti-inflammatory properties.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Succinobucol is a novel derivative of probucol with improved antioxidant and anti-inflammatory properties." | ( Succinobucol-eluting stents increase neointimal thickening and peri-strut inflammation in a porcine coronary model. Agbani, EO; Behnisch, B; Czudaj, P; Kennedy, S; McCormick, C; McPhaden, A; Mullen, A; Oldroyd, KG; Wadsworth, RM; Watt, J, 2013) | 2.55 |
Treatment
| Excerpt | Reference | Relevance |
|---|---|---|
| "Succinobucol pretreatment (6 days) significantly prevented 3-NP-induced loss of cellular viability, generation of reactive oxygen species, and decrease of ΔΨm." | ( Succinobucol, a Lipid-Lowering Drug, Protects Against 3-Nitropropionic Acid-Induced Mitochondrial Dysfunction and Oxidative Stress in SH-SY5Y Cells via Upregulation of Glutathione Levels and Glutamate Cysteine Ligase Activity. Braga, AL; Colle, D; de Bem, AF; Engel, DF; Farina, M; Godoi, M; Hartwig, JM; Santos, DB, 2016) | 2.6 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| " AGI-1067 is the metabolically stable monosuccinic acid ester of probucol, and a potent phenolic antioxidant representing a novel class of orally bioavailable compounds termed vascular protectants." | ( AGI-1067, a novel vascular protectant, anti-inflammatory drug and mild antiplatelet agent for treatment of atherosclerosis. Eisert, C; Malinin, A; Ong, S; Serebruany, VL, 2007) | 0.34 |
| "Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported." | ( Succinobucol's new coat--conjugation with steroids to alter its drug effect and bioavailability. Buřičová, L; Drašar, P; Galandáková, A; Horníček, J; Ikonen, S; Jurček, O; Kolehmainen, ET; Ulrichová, J; Wimmer, Z; Wimmerová, M, 2011) | 2 |
| " Furthermore, the oral bioavailability of SCB was greatly improved about 13-fold by SN, and the biodistribution in major organs was evidently enhanced." | ( Hydrophobic interaction mediating self-assembled nanoparticles of succinobucol suppress lung metastasis of breast cancer by inhibition of VCAM-1 expression. Cao, H; Chen, L; Gu, W; He, X; Li, Y; Yin, Q; Yu, H; Zhang, Z; Zhao, S, 2015) | 0.65 |
Dosage Studied
| Excerpt | Relevance | Reference |
|---|---|---|
| "02 for the dose-response relationship; P< or =0." | ( Effects of AGI-1067 and probucol after percutaneous coronary interventions. Bourassa, MG; Glass, M; Grégoire, J; Guertin, MC; L'Allier, PL; Lambert, J; Laramée, L; Lespérance, J; Reeves, F; Schwartz, L; Tardif, JC; Title, L, 2003) | 0.32 |
| " These data need to be confirmed in subjects receiving orally dosed AGI-1067 to be clinically relevant." | ( The in vitro effects of a novel vascular protectant, AGI-1067, on platelet aggregation and major receptor expression in subjects with multiple risk factors for vascular disease. Malinin, A; Scott, R; Serebruany, V, 2006) | 0.33 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (2)
| Class | Description |
|---|---|
| benzoate ester | Esters of benzoic acid or substituted benzoic acids. |
| phenols | Organic aromatic compounds having one or more hydroxy groups attached to a benzene or other arene ring. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
Protein Targets (1)
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Vascular cell adhesion protein 1 | Homo sapiens (human) | IC50 (µMol) | 6.0000 | 6.0000 | 6.5000 | 7.0000 | AID216494 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (26)
Molecular Functions (4)
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| integrin binding | Vascular cell adhesion protein 1 | Homo sapiens (human) |
| primary amine oxidase activity | Vascular cell adhesion protein 1 | Homo sapiens (human) |
| cell adhesion molecule binding | Vascular cell adhesion protein 1 | Homo sapiens (human) |
| cell adhesion mediator activity | Vascular cell adhesion protein 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
Ceullar Components (14)
Bioassays (8)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID224019 | Inhibition of progression of atherosclerosis in aorta after oral dosing in cholesterol fed rabbits | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| AID135188 | Inhibition of progression of atherosclerosis in aorta after oral dosing in cholesterol fed LDL receptor knockout mice | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| AID216494 | Inhibition of TNF-alpha inducible Vascular cell adhesion molecule-1 expression. | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| AID202571 | Concentration required for 50% inhibition of TNF-alpha inducible Selectin E expression. | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| AID227564 | Inhibitory effect in preventing the oxidation of linoleic acid by 15-lipoxygenase at a concentration of 70 uM | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| AID281899 | Inhibition of TNF-alpha-stimulated VCAM1 expression in endothelial cells | 2004 | Journal of medicinal chemistry, Dec-02, Volume: 47, Issue:25 | Discovery of novel phenolic antioxidants as inhibitors of vascular cell adhesion molecule-1 expression for use in chronic inflammatory diseases. |
| AID89971 | Inhibition of proliferation of human aortic smooth muscle cells at a concentration of 5 uM | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| AID104100 | Concentration required for 50% inhibition of TNF-alpha inducible MCP-1 expression. | 2002 | Bioorganic & medicinal chemistry letters, Sep-16, Volume: 12, Issue:18 | Novel phenolic antioxidants as multifunctional inhibitors of inducible VCAM-1 expression for use in atherosclerosis. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (52)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 33 (63.46) | 29.6817 |
| 2010's | 19 (36.54) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 19.58
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (19.58) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (9.43%) | 5.53% |
| Reviews | 17 (32.08%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 31 (58.49%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||