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Cat. No.: HY-189271

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Anti-neuroinflammation agent-4

Anti-neuroinflammation agent-4 is a blood-brain barrier-penetrating inhibitor of IκBα, NLRP3, and NF-κB p65. Anti-neuroinflammation agent-4 exerts anti-neuroinflammatory effects by inhibiting IκBα phosphorylation, reducing NLRP3 and caspase-1 expression, and suppressing p65 phosphorylation and its nuclear translocation, thereby decreasing the release of inflammatory mediators such as ROS, NO, IL-1β, IL-6, TNF-α, and IL-18 in microglia. Anti-neuroinflammation agent-4 can be used for research on neuroinflammation.

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

CAS No.: 3113312-38-9
Formula: C₃₁H₃₃N₃O₃
Molecular Weight:495.61

Storage:

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

Anti-neuroinflammation agent-4 Chemical Structure

CAS No.: 3113312-38-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

NLRP3

NF-κB

IL-1β

IL-6

IL-18

Caspase-1

IκBα

TNF-α

All NOD-like Receptor (NLR) Isoforms :

All NF-κB Isoforms :

All Caspase Isoforms :

All NO Synthase Isoforms :

All Interleukin Related Isoforms :

All TNF Receptor Isoforms :

In Vitro

Anti-neuroinflammation agent-4 (compound 10a) (10.0 μM; 2 h) exhibits strong anti-inflammatory activity in LPS-induced BV2 microglia by inhibiting the release of TNF-α and IL-6^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 2 h) inhibits the release of pro-inflammatory cytokines IL-6, TNF-α, IL-1β, and IL-18 in a dose-dependent manner in LPS-induced BV2 microglial cells^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 2 h) ameliorates neuroinflammation in BV2 microglia by inhibiting the NF-κB/NLRP3 signaling pathway^[1].
Anti-neuroinflammation agent-4 (1-40 μM; 24 h) exhibits safety properties in BV2 microglial cells up to a concentration of 12.0 μM^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 24 h) is safe at concentrations up to 12.0 μM and does not cause significant death of BV2 microglial cells^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 2 h) reduces LPS-induced NO production in BV2 microglia in a dose-dependent manner^[1].
Anti-neuroinflammation agent-4 (12.0 μM; 24 h) inhibits the nuclear translocation of NF-κB p65 in LPS-stimulated BV2 microglia^[1].
Anti-neuroinflammation agent-4 (10.0 μM) exhibits extremely low cytotoxicity in BV2 microglial cells, with a survival rate of 95.9%^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 24 h) does not induce significant apoptosis in BV2 microglial cells at concentrations up to 12.0 μM^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 2 h) reduces ROS production in LPS-induced BV2 microglial cells in a dose-dependent manner, as observed by fluorescence microscopy^[1].
Anti-neuroinflammation agent-4 (3.0-12.0 μM; 2 h) reduces LPS-induced ROS production in BV2 microglia in a dose-dependent manner^[1].

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

ELISA Assay^[1]

Cell Line:

BV2 microglial cells
Concentration:

10.0 μM
Incubation Time:

2 h
Result:

Exhibited 55.8% inhibition of TNF-α.
Exhibited 72.1% inhibition of IL-6.

Cell Viability Assay^[1]

Cell Line:

BV2 microglial cells
Concentration:

1, 3, 6, 9, 12, 18, 24, 30, 40 μM
Incubation Time:

24 h
Result:

Did not cause significant cytotoxicity, with cell viability remaining above 80% at 12.0 μM.

Cell Cytotoxicity Assay^[1]

Cell Line:

BV2 microglial cells
Concentration:

3.0, 6.0, 12.0 μM
Incubation Time:

24 h
Result:

The proportion of dead cells was less than 5% at 12.0 μM.

Apoptosis Analysis^[1]

Cell Line:

BV2 microglial cells
Concentration:

3.0, 6.0, 12.0 μM
Incubation Time:

24 h
Result:

The percentage of viable cells in the 12.0 μM group was more than 90%, with an early apoptotic rate of 1.01%.

ELISA Assay^[1]

Cell Line:

BV2 microglial cells
Concentration:

3.0, 6.0, 12.0 μM
Incubation Time:

2 h
Result:

Effectively downregulated the inflammation levels (IL-6, TNF-α, IL-18, and IL-1β) in a dose-dependent manner.

Immunofluorescence^[1]

Cell Line:

BV2 microglial cells
Concentration:

3.0, 6.0, 12.0 μM
Incubation Time:

2 h
Result:

The fluorescence intensities gradually decreased with increasing 10a concentrations, indicating that 10a efficiently decreased the oxidative stress induced by LPS.

Immunofluorescence^[1]

Cell Line:

BV2 microglial cells
Concentration:

12.0 μM
Incubation Time:

24 h
Result:

Partially reduced the nuclear accumulation of p65, indicating that 10a inhibited NF-κB nuclear translocation upon LPS stimulation.

Western Blot Analysis^[1]

Cell Line:

BV2 microglial cells
Concentration:

3.0, 6.0, 12.0 μM
Incubation Time:

2 h
Result:

Significantly attenuated the phosphorylation levels of NF-κB p65 and IκBα without altering their total protein abundance.
Suppressed the LPS-induced upregulation of NLRP3 and caspase-1 protein levels in a dose-dependent manner.

Chemical Information

CAS No. 3113312-38-9
Molecular Weight 495.61
Formula C₃₁H₃₃N₃O₃
SMILES

COC1=C2C(OCCC3=C2NC(C4=CC=CC=C4)=NC3C5=CC=C(N6CCCCC6)C=C5)=CC(OC)=C1
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]. Xia DL, et al. 1,4,5,6-Tetrahydrobenzo[2,3]oxepino[4,5-d]pyrimidine derivatives as anti-neuroinflammatory agents: Design, synthesis, and preliminary biological evaluation. Bioorganic chemistry. 2026 Oct 05;181:110360.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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Anti-neuroinflammation agent-4

All NOD-like Receptor (NLR) Isoforms

All NF-κB Isoforms

All Caspase Isoforms

All NO Synthase Isoforms

All Interleukin Related Isoforms

All TNF Receptor Isoforms