Neuroprotective agent 10
Neuroprotective agent 10 is an orally active, blood-brain barrier permeable neuroprotective agent. Neuroprotective agent 10 scavenges ABTS, DPPH and superoxide anion free radicals. Neuroprotective agent 10 inhibits abnormal electrical discharges. At the cellular level, Neuroprotective agent 10 alleviates H2O2-induced oxidative damage and LPS (HY-D1056)-induced neuroinflammation, and relieves epileptic symptoms and oxidative damage in mice. Neuroprotective agent 10 can be used in the research of epilepsy.
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- Formule: C17H27N3O3
- Masse moléculaire:321.41
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Neuroprotective agent 10 (Compound 11c) potently scavenges ABTS, DPPH and superoxide anion radicals in cell-free assays, with IC50 values of 92.0 μM, 70.9 μM, and an inhibition rate of 48.4% (at a concentration of 2.5 mM)[1].
Neuroprotective agent 10 (10-100 μM; 24 h) exhibits no cytotoxicity against HT22 mouse hippocampal neuronal cells at a concentration of 50.0 μM, but reduces cell viability to 88.8% of that in the control group after 24 h of incubation at a concentration of 100.0 μM[1].
Neuroprotective agent 10 (10-100 μM; 24 h) significantly protects HT22 mouse hippocampal neurons against H2O2-induced damage at a concentration of 50.0 μM, and reduces cell damage by 36.0% in a dose-dependent manner[1].
Neuroprotective agent 10 (2.5-50 μM; 24 h) potently inhibits lipopolysaccharide (LPS)-induced nitric oxide (NO) release by up to 92.5% and tumor necrosis factor-α (TNF-α) release by up to 76.2% in a dose-dependent manner in BV-2 mouse microglial cells[1].
Neuroprotective agent 10 (50 μM; 8.5 h) potently inhibits LPS-induced reactive oxygen species (ROS) production in BV-2 mouse microglia at a concentration of 50.0 μM, with an inhibition rate of 91.2%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT22 mouse hippocampal neuronal cells
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Concentration:10, 50 and 100 μM
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Incubation Time:24 h
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Result:Reduced H2O2-induced cell damage by 36.0% in a dose-dependent manner at 50.0 μM.
Showed lower cell viability at 100.0 μM than at 50.0 μM, likely due to combined neuroprotective and cytotoxic effects.
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Cell Line:LPS-activated BV-2 mouse microglial cells
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Concentration:50 μM
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Incubation Time:8 h preincubation, followed by 30 min LPS co-incubation
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Result:Inhibited LPS-induced ROS production by 91.2% at 50.0 μM.
| Species | Dose | Route | Cmax (Brain) | Tmax (Brain) | T1/2 (Brain) | Cmax | Tmax (Plasma) | T1/2 (Plasma) | AUC0-t |
|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 50.0 mg/kg | i.g. | 2.4 μg/g | 0.5 h | 3.5 h | 14.5 μg/mL | 0.5 h | 3.6 h | 39.1 mg/h/L |
Compound 11c (50.0 mg/kg; i.g.; single administration) exhibits significant anticonvulsant activity in pilocarpine (HY-B0726A)-induced epileptic model mice[1].
Compound 11c (50.0 mg/kg; i.g.; once daily; for 4 consecutive weeks) exhibits potent in vivo antioxidant activity in mice with oxidative stress induced by Sodium Nitrite (HY-N11218), which reduces MDA levels, enhances SOD activity and alleviates neuronal damage[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J (adult male, pentylenetetrazole-induced clonic seizures)[1]
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Dosage:50.0 mg/kg
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Administration:i.g.; single administration 60 minutes prior to PTZ challenge
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Result:Extended the latency to the first clonus by 141.7%.
Reduced the number of seizure episodes by 50.0%.
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Animal Model:C57BL/6 J (adult male, pilocarpine-induced tonic-clonic seizures)[1]
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Dosage:50.0 mg/kg
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Administration:i.g.; single administration 60 minutes prior to pilocarpine challenge
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Result:Extended the latency to status epilepticus by 138.1%.
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Animal Model:C57BL/6 J (adult male, sodium nitrite-induced oxidative stress)[1]
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Dosage:50.0 mg/kg
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Administration:i.g.; once daily; 4 weeks
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Result:Reduced cerebral cortex MDA content.
Increased cerebral cortex SOD activity.
Improved hippocampal neuronal damage observed via immunohistochemical staining.
Chemical Information
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Masse moléculaire 321.41
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Formule C17H27N3O3
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SMILES
OC1=C(OC)C=C(CNCCCN2CCCC(C(N)=O)C2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Neuroprotective agent 10 Related Classifications
HY-172604 Related Classifications
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- Neuroprotective agent 10
- Neuroprotective agent10
- Neuroprotective agent-10
- Free Radical Scavengers
- Reactive Oxygen Species (ROS)
- TNF Receptor
- pilocarpine-induced seizure model mice
- pentylenetetrazole-induced seizure model mice
- neuroinflammation
- BV-2 mouse microglial cells
- HT22 mouse hippocampal neuronal cells
- oxidative damage
- DPPH radicals
- ABTS radicals
- superoxide anion radicals
- epilepsy
- Inhibitor
- inhibitor
- inhibit