NSP-116
NSP-116 is an orally active antioxidant and neuroprotective agent. NSP-116 protects corneal epithelial cells from UV-A and blue light LED-induced photo-oxidative damage. NSP-116 scavenges DPPH, superoxide anion, and hydroxyl radicals, inhibits light-induced ROS production in photoreceptor cells, and inhibits lipid peroxidation in retinal homogenates. NSP-116 prevents light-induced photoreceptor cell death and retinal degeneration, and inhibits intracellular Fe2+ accumulation, autophagy, apoptosis, p38 phosphorylation, and microglial/macrophage activation. NSP-116 exerts neuroprotective effects in hemorrhagic stroke models. NSP-116 can be used for research on photokeratitis, dry age-related macular degeneration, and intracranial hemorrhage.
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- No. CAS: 1643925-08-9
- Fòrmula: C15H19N5O
- Peso molecular:285.34
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Actividad biológica
Descripciòn
In Vitro
NSP-116 (0.1-10 μM; 1 h) significantly inhibits light-induced ROS production in 661 W cells[2].
NSP-116 (3-100 μM; 30 min) exhibits significant DPPH radical scavenging activity[2].
NSP-116 (1 min) exhibits potent scavenging activity against DPPH, •O2−, and •OH radicals[2].
NSP-116 (10-100 μM; 1 h) significantly reduces lipid peroxidation production in porcine retinal tissue homogenates[2].
NSP-116 (10 μM; 1 h) inhibits UV-A- or blue light LED-induced stress response signaling pathways in HCE-T cells[1].
NSP-116 (0.1-10 μM; 1 h) significantly inhibits light-induced cell death in 661 W cells[2].
NSP-116 (0.1-10 μM; 1 h) significantly inhibits the light-induced decrease in cell viability in 661 W cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCE-T
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Concentration:1, 3, 10 μM (NSP-116); 16.2 μM (Hoechst 33342); 1.5 μM (PI)
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Incubation Time:1 h (NSP-116); 0.5 h (UV-A light exposure); 24 h (blue LED light exposure); 30 min (Hoechst 33342/PI staining); 2 h (CCK-8)
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Result:Reduced UV-A-induced cell death rate from 27.1% to 17.3% at 10 μM.
Inhibited UV-A-induced reduction in cell viability at 10 μM.
Reduced blue LED light-induced cell death rate from 7.8% to 2.6% at 10 μM.
Inhibited blue LED light-induced reduction in cell viability at 10 μM.
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Cell Line:HCE-T
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Concentration:10 μM
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Incubation Time:1 h
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Result:Inhibited phosphorylation of p38 MAPK induced by UV-A light at 10 μM.
Inhibited phosphorylation of p38 MAPK induced by blue LED light at 10 μM.
Inhibited phosphorylation of NF-κB induced by UV-A light at 10 μM.
Inhibited phosphorylation of NF-κB induced by blue LED light at 10 μM.
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Cell Line:661 W cells
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Concentration:0.1, 1, 3, 10 μM
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Incubation Time:1 h
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Result:Inhibited the reduction in cell viability at 3 and 10 μM.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ddY mice (male, 7 weeks old)[1]
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Dosage:10 μM
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Administration:Eye drops; twice daily; 10 days
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Result:Inhibited the increase of TUNEL-positive cells to 2.5 cells per 1000 μm corneal arc in the whole cornea, compared to the vehicle group which had 3.3 cells per 1000 μm corneal arc.
Suppressed TUNEL-positive cells significantly on the upper side of the cornea (Vehicle group: 4.1 cells/1000 μm; NSP-116 group: 2.2 cells/1000 μm).
Had no effect on apoptosis in the lower side of the cornea.
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Animal Model:ddY mice (eight-week-old, male)[2]
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Dosage:10 or 30 mg/kg
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Administration:p.o.; single dose; 30 min before light exposure
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Result:Protected against the reduction in the a-wave amplitude induced by light exposure compared with the vehicle-treated group.
Showed a tendency to suppress the reduction in the b-wave amplitudes.
Suppressed the light-induced ONL thinning compared with the vehicle-treated group.
- Western Blot
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Kinase activity and phosphorylation assays
- Phagocytosis Functional Assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Cell Cytotoxicity Assay
- Autophagy
- Apoptosis Solutions
- Ferroptosis Solutions
- Lysosome and acidic-vesicle live-cell staining
- Protocol for Kinase activity and phosphorylation assays
- Macroautophagy Solutions
Chemical Information
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No. CAS 1643925-08-9
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Peso molecular 285.34
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Fòrmula C15H19N5O
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SMILES
O=C(C)N1CCN(CC1)C2=CC=C(C(N3C=NC=C3)=C2)N
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NSP-116 Related Classifications
HY-189150 Related Classifications
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