PeptideDB

Antioxidant agent-8

Antioxidant agent-8

CAS No.:

Antioxidant agent-8 is an orally bioactive Aβ1-42 deposition inhibitor. Antioxidant agent-8 inhibits fibril aggregation
Data collection:peptidedb@qq.com

This product is for research use only, not for human use. We do not sell to patients.

Antioxidant agent-8 is an orally bioactive Aβ1-42 deposition inhibitor. Antioxidant agent-8 inhibits fibril aggregation (IC50=11.15 µM) and promotes fibril decomposition (IC50=6.87 µM). Antioxidant agent-8 also inhibits Cu2+-induced Aβ1-42 fibril aggregation (IC50=3.69 µM) and promotes Cu2+-induced Aβ1-42 fibril decomposition (IC50=3.35 µM). Antioxidant agent-8 displays anti-oxidant effect, anti-inflammatory activity, biosafety, BBB (blood-brain barrier) permeability, and neuro-protection effects.

Physicochemical Properties


Molecular Formula C13H12O5
Molecular Weight 248.23
Appearance Typically exists as solid at room temperature
HS Tariff Code 2934.99.9001
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)

Biological Activity


ln Vitro Compound 30, or antioxidant agent-8, at 50 µM for 24 hours, effectively chelates metal ions such as Cu2+, Fe2+, Zn2+, Fe3+, and Al3+. This results in a considerable reduction in self- and Cu2+-induced aggregation and degradation of Aβ1-42 fibrils [1]. In a concentration-dependent way, antioxidant agent-8 (2.5, 5 and 10 µM; 24 h) decreases Aβ1-42-induced apoptosis, increases the clearance of Aβ1-42 by BV-2 cells, and preserves nerves [1].
ln Vivo Compound 30, or antioxidant agent-8, shows hemorrhagic brain permeability and accumulation in the hippocampus at a dose of 15 mg/kg intraperitoneally [1]. Antioxidant agent-8 has proven to be biosafe (2000 mg/kg; intraperitoneal injection; single dosage) [1]. Antioxidant agent-8 (20 mg/kg; oral dose; once daily for 25 days) markedly reduced the effects of scopolamine (HY-N0296) on anxiety, memory, and cognitive function [1].
Cell Assay Western Blot Analysis[1]
Cell Types: Mouse microglia BV-2 cells.
Tested Concentrations: 2.5, 5 and 10 µM.
Incubation Duration: 24 h.
Experimental Results: decreased the expression level of Aβ1-42 in cells.

Apoptosis Analysis[1]
Cell Types: Mouse microglia BV-2 cells.
Tested Concentrations: 2.5, 5 and 10 µM.
Incubation Duration: 24 h.
Experimental Results: Dramatically decreased Aβ1-42 induced apoptosis(cell apoptosis rate were below 30%).

Cell Viability Assay[1]
Cell Types: Mouse microglia BV-2 cells.
Tested Concentrations: 2.5, 5 and 10 µM.
Incubation Duration: 24 h.
Experimental Results: Promoted cell viability and the cell survival was 75.50 %(10 µM).
Animal Protocol Animal/Disease Models: SD (Sprague-Dawley) rats[1].
Doses: 15 mg/kg.
Route of Administration: intragastric (po) administration; single dose.
Experimental Results: Appeared in plasma and hippocampus at 0.083, 0.167, 0.25, 0.5, 1, 2 and 4 hrs (hours) after administration , and then gradually gathered in hippocampus.

Animal/Disease Models: Mice[1].
Doses: 2000 mg/kg.
Route of Administration: intragastric (po) administration; single dose.
Experimental Results: demonstrated insignificant toxic and side effects on heart, liver, spleen and brain.

Animal/Disease Models: SCOP-induced cognitive impairment in ICR mice (25-28 g)[1].
Doses: 20 mg/kg.
Route of Administration: po (oral gavage); from day 7 to day 31, after 30 min of SCOP administration.
Experimental Results: Improved animal behavior , learning and memory.
References [1]. Liu X, et al. Novel neuroprotective pyromeconic acid derivatives with concurrent anti-Aβ deposition, anti-inflammatory, and anti-oxidation properties for treatment of Alzheimer's disease. Eur J Med Chem. 2023 Feb 15;248:115120.

Solubility Data


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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.0285 mL 20.1426 mL 40.2852 mL
5 mM 0.8057 mL 4.0285 mL 8.0570 mL
10 mM 0.4029 mL 2.0143 mL 4.0285 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.