Neuroprotective agent 20
Neuroprotective agent 20 is an α-lipoic acid-derived neuroprotective agent that possesses both ferroptosis-inhibitory activity and anti-inflammatory activity. Neuroprotective agent 20 has an anti-ferroptosis EC50 = 0.00247 μM and an anti-inflammatory IC50 = 13.6 μM. Neuroprotective agent 20 scavenges free radicals, activates the Nrf2/GPX4 pathway to elevate GSH levels, and reduces MDA and ROS accumulation, thereby inhibiting ferroptosis. Neuroprotective agent 20 inhibits NF-κB activation by preventing IκBα degradation and p65 phosphorylation, and suppresses the secretion of IL-1β, IL-6, and TNF-α. Neuroprotective agent 20 reduces cerebral infarct volume and ameliorates neurological deficits in a rat model of middle cerebral artery occlusion ischemic stroke. Neuroprotective agent 20 can be used for research on ischemic stroke.
For research use only. We do not sell to patients.
- Formula: C26H31N3O2S3
- Molecular Weight:513.74
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
IL-1β |
IL-6 |
TNF-α |
NF-κB |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-12 | EC50 |
0.00247 μM
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Inhibition of erastin-induced ferroptosis in PC12 cells assessed as viability by CCK-8 assay after 24 hrs exposure.
Inhibition of erastin-induced ferroptosis in PC12 cells assessed as viability by CCK-8 assay after 24 hrs exposure.
|
acs.jmedchem.6c00739 |
| BV-2 | IC50 |
13.6 μM
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Inhibition of LPS-induced nitric oxide release in BV2 cells measured by nitric oxide assay kit after 24 hrs exposure.
Inhibition of LPS-induced nitric oxide release in BV2 cells measured by nitric oxide assay kit after 24 hrs exposure.
|
acs.jmedchem.6c00739 |
In Vitro
Neuroprotective agent 20 (0.01-1 μM; 24 h) antagonizes Erastin-induced ferroptosis markers in PC12 cells, increases GSH, and decreases MDA, Fe2+, and ROS[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells
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Concentration:1 μM
mixed with 4 μM (Erastin) -
Incubation Time:24 h
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Result:Erastin decreased Nrf2 and GPX4 protein levels.
Restored both Nrf2 and GPX4 protein expression and increased Nrf2 and GPX4 immunofluorescence intensities.
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Cell Line:BV2 cells
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Concentration:15 μM
1 μg/mL (LPS) -
Incubation Time:24 h
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Result:Prevented IκBα degradation, reduced the p-p65/p65 ratio, and decreased nuclear p65 and p-p65 immunofluorescence signals.
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Cell Line:BV2 cells
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Concentration:15 μM
1 μg/mL (LPS) -
Incubation Time:24 h
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Result:Reduced IL-1β, IL-6, and TNF-α secretion.
Parmacokinetics
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Vd | CL | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 0.359 h | 0.0833 h | 461 ng/mL | 145 ng·h/mL | 146 ng·h/mL | 3.65 L/kg | 116.3 mL/min/kg | 0.198 h | 0.224 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 250-300 g, approximately 250 g at study)[1]
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Dosage:5 mg/kg
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Administration:i.v.; single administration after 1.5 h MCAO; 24 h reperfusion
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Result:Reduced cerebral infarct volume relative to vehicle and produced the greatest infarct-volume reduction among the tested treatments, surpassing ALA and EDV.
Improved neurological deficit scores relative to vehicle and showed greater functional recovery than EDV.
In the ipsilateral hemisphere, increased GSH and reduced MDA and Fe2+ relative to vehicle, with greater efficacy than EDV.
Also reduced IL-1β, IL-6, and TNF-α relative to vehicle, with superior anti-inflammatory activity compared with EDV.
- Kinase activity and phosphorylation assays
- Western Blot
- Cotton Pellet Granuloma
- ROS/oxidative-stress fluorescent staining
- Carrageenan-Induced Paw Edema
- How to Select a Suitable Non-Mouse Animal Model
- Ferroptosis Solutions
- Research Protocol for Inflammation-related Diseases
- Protocol for Kinase activity and phosphorylation assays
- Pyroptosis Solutions
- How to Choose the Right Model Animal
Chemical Information
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Molecular Weight 513.74
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Formula C26H31N3O2S3
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SMILES
O=C(C1CC(NC(CCCCC2CCSS2)=O)C1)NCC3=CC4=C(C=C3)SC5=CC=CC=C5N4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Neuroprotective agent 20
- Neuroprotective agent20
- Neuroprotective agent-20
- Ferroptosis
- Keap1-Nrf2
- Reactive Oxygen Species (ROS)
- NF-κB
- NO Synthase
- Interleukin Related
- TNF Receptor
- Nuclear factor-κB
- Nuclear factor-kappaB
- Nitric oxide synthases
- NOS
- IL
- Tumor Necrosis Factor Receptor
- TNFR
- GPX4
- IL-1β
- IL-6
- Nrf2
- PC12 cells
- TNF-α
- ferroptosis
- ischemic stroke
- lipid peroxidation
- Inhibitor
- inhibitor
- inhibit