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| Targets |
Camobucol's mechanism of action involves multiple targets. It is a potent antioxidant that inhibits LDL oxidation and reduces lipid peroxidation. It also inhibits vascular cell adhesion molecule-1 (VCAM-1) expression, which is a key step in the recruitment of inflammatory cells to the vascular endothelium. This dual mechanism, combining antioxidant and anti-inflammatory effects, contributes to its potential therapeutic benefits.
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| ln Vitro |
Camobucol demonstrates increased cellular absorption and strong antioxidant action against lipid peroxides in vitro. Camobucol has a lesser inhibitory effect on E-selectin but selectively reduces the levels of redox-sensitive genes, vascular cell adhesion molecule-1, and monocyte chemoattractant protein-1 generated by tumor necrosis factor (TNF)-α. There is no impact from intracellular adhesion molecules. Within endothelial cells, 1 is expressed. Furthermore, camobucol prevents lipopolysaccharide-induced TNF-α and IL-release as well as cytokine-induced levels of monocyte chemoattractant protein-1, interleukin (IL)-6, and IL-8 in endothelial cells and human fibroblast-like synoviocytes. From human peripheral blood mononuclear cells, 1β and IL-6 are produced. The mechanism of action of camobucol is independent of the redox-sensitive transcription factor NF-κB, as evidenced by its inability to block TNF-α-induced nuclear translocation of NF-κB in B cells [1].
In vitro, Camobucol exhibits potent antioxidant activity toward lipid peroxides. It displays enhanced cellular uptake. It demonstrates strong antioxidant properties, effectively combating lipid peroxides. It also shows improved absorption by cells. Its ability to inhibit VCAM-1 expression further supports its anti-inflammatory activity in vitro. |
| ln Vivo |
In vivo, Camobucol is an orally active compound. It has been studied for its antirheumatic properties. Its actions encompass modulation of lipoprotein catabolism, potent antioxidant effects, and anti-inflammatory properties. Its ability to inhibit LDL oxidation and reduce lipid peroxidation suggests it could have beneficial effects in atherosclerosis and other inflammatory diseases.
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| Enzyme Assay |
The in vitro antioxidant activity of Camobucol is typically assessed using cell-free assays. In a standard protocol, the compound is incubated with a source of lipid peroxides, such as LDL or a model membrane system. The formation of lipid peroxidation products (e.g., malondialdehyde) is measured, and the compound's ability to inhibit this process is determined.
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| Cell Assay |
Cellular assays for Camobucol involve studying its effects on inflammatory responses in cells. In a typical protocol, endothelial cells are stimulated with an inflammatory cytokine (e.g., TNF-α) to induce VCAM-1 expression. The cells are treated with Camobucol, and the level of VCAM-1 expression is measured by flow cytometry or ELISA. The compound's ability to inhibit VCAM-1 expression is assessed.
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| Animal Protocol |
The in vivo efficacy of Camobucol can be evaluated in animal models of inflammatory diseases, such as arthritis or atherosclerosis. In these studies, the compound is administered orally to animals. The primary endpoints are the reduction in disease severity, as measured by clinical scores, histopathological analysis, or biomarkers of inflammation. These studies confirm its in vivo anti-inflammatory and antioxidant activity.
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| ADME/Pharmacokinetics |
Camobucol has a molecular weight of 574.88 and a molecular formula of C₃₃H₅₀O₄S₂. It is an orally active, small-molecule phenolic antioxidant. As a research compound, detailed pharmacokinetic data are not typically reported in the public domain, but its oral bioavailability makes it suitable for in vivo studies. Its properties are well-suited for use in preclinical models of inflammatory diseases.
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| Toxicity/Toxicokinetics |
The safety and toxicity of Camobucol would be assessed in standard preclinical toxicology studies. As an antioxidant and anti-inflammatory compound, its toxicity profile is expected to be related to its mechanism of action. Its safety would be carefully evaluated during drug development to determine its therapeutic index.
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| References |
[1]. Kunsch C, et al. AGIX-4207 [2-[4-[[1-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]thio]-1-methylethyl]thio]-2,6-bis(1,1-dimethylethyl)phenoxy]acetic acid], a novel antioxidant and anti-inflammatory compound: cellular and biochemical characterization of an
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| Additional Infomation |
Camobucol (AGIX-4207) is an orally active, phenolic antioxidant and anti-inflammatory compound. It has antirheumatic properties and acts by inhibiting LDL oxidation and reducing lipid peroxidation. It also inhibits VCAM-1 expression. It is a research compound being investigated for the treatment of inflammatory diseases, but it is not an approved drug.
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| Molecular Formula |
C33H50O4S2
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| Molecular Weight |
574.88
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| Exact Mass |
574.315
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| CAS # |
216167-92-9
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| PubChem CID |
9875498
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
9.666
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
39
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| Complexity |
764
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C)(C)C1=CC(SC(C)(C)SC2=CC(C(C)(C)C)=C(OCC(O)=O)C(C(C)(C)C)=C2)=CC(C(C)(C)C)=C1O
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| InChi Key |
FGBGXESDYFKUFX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C33H50O4S2/c1-29(2,3)22-15-20(16-23(27(22)36)30(4,5)6)38-33(13,14)39-21-17-24(31(7,8)9)28(37-19-26(34)35)25(18-21)32(10,11)12/h15-18,36H,19H2,1-14H3,(H,34,35)
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| Chemical Name |
2-[2,6-ditert-butyl-4-[2-(3,5-ditert-butyl-4-hydroxyphenyl)sulfanylpropan-2-ylsulfanyl]phenoxy]acetic acid
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| Synonyms |
Camobucol (USAN/INN); UNII-FZ7798X3IR; Camobucol
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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 | 1.7395 mL | 8.6975 mL | 17.3949 mL | |
| 5 mM | 0.3479 mL | 1.7395 mL | 3.4790 mL | |
| 10 mM | 0.1739 mL | 0.8697 mL | 1.7395 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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