Antioxidant agent-8

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Antioxidant agent-8 is an orally active inhibitor of Aβ_1-42 deposition. Antioxidant agent-8 inhibits fibril aggregation (IC₅₀=11.15 µM) and promotes fibril disaggregation (IC₅₀=6.87 µM). Antioxidant agent-8 also inhibits Cu²⁺-induced Aβ_1-42 fibril aggregation (IC₅₀=3.69 µM) and promotes Cu²⁺-induced Aβ_1-42 fibril disaggregation (IC₅₀=3.35 µM). Antioxidant agent-8 has antioxidant activity, anti-inflammatory activity, biosafety, blood-brain barrier permeability and neuroprotective effect.

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

Antioxidant agent-8 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

Antioxidant agent-8 (compound 30) (50 µM; 24 h) selectively chelates with Cu²⁺, Fe²⁺, Zn²⁺, Fe³⁺ and Al³⁺ metal ions, significantly inhibits self- and Cu²⁺-induced Aβ_1-42 fibril aggregation and disaggregation^[1].
Antioxidant agent-8 (2.5, 5 and 10 µM; 24 h) promotes BV-2 cells to clear Aβ_1-42, reduces Aβ_1-42 induced apoptosis and protects nerves with concentration-dependent manner^[1].

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

Western Blot Analysis^[1]

Cell Line:	Mouse microglia BV-2 cells.
Concentration:	2.5, 5 and 10 µM.
Incubation Time:	24 h.
Result:	Reduced the expression level of Aβ_1-42 in cells.

Apoptosis Analysis^[1]

Cell Line:	Mouse microglia BV-2 cells.
Concentration:	2.5, 5 and 10 µM.
Incubation Time:	24 h.
Result:	Significantly reduced Aβ_1-42 induced apoptosis (cell apoptosis rate were below 30%).

Cell Viability Assay^[1]

Cell Line:	Mouse microglia BV-2 cells.
Concentration:	2.5, 5 and 10 µM.
Incubation Time:	24 h.
Result:	Promoted cell viability and the cell survival was 75.50 % (10 µM).

In Vivo

Antioxidant agent-8 (compound 30) (15 mg/kg; i.g.; single dose) shows blood-brain barrier permeability and accumulates in the hippocampus^[1].
Antioxidant agent-8 (2000 mg/kg; i.g.; single dose) exhibits biosafety^[1].
Antioxidant agent-8 (20 mg/kg; p.o.; once daily for 25 d) significantly improves anxiety, memory impairment and cognitive impairment caused by Scopolamine (HY-N0296)^[1].

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

Animal Model:	Sprague-Dawley rats^[1].
Dosage:	15 mg/kg.
Administration:	Intragastric administration; single dose.
Result:	Appeared in plasma and hippocampus at 0.083, 0.167, 0.25, 0.5, 1, 2 and 4 hours after administration, and then gradually gathered in hippocampus.

Animal Model:	Mice^[1].
Dosage:	2000 mg/kg.
Administration:	Intragastric administration; single dose.
Result:	Showed insignificant toxic and side effects on heart, liver, spleen and brain.

Animal Model:	SCOP-induced cognitive impairment in ICR mice (25-28 g)^[1].
Dosage:	20 mg/kg.
Administration:	Oral gavage; from day 7 to day 31, after 30 min of SCOP administration.
Result:	Improved animal behavior, learning and memory.

Molecular Weight

248.23

Formula

C₁₃H₁₂O₅

SMILES

O=C1CCOC(/C=C/C2=CC=C(C(O)=C2)O)=C1O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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. [Content Brief]