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Cat. No.: HY-189150

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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.

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

CAS No.: 1643925-08-9
Formula: C₁₅H₁₉N₅O
Molecular Weight:285.34

Storage:

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

NSP-116 Chemical Structure

CAS No.: 1643925-08-9

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Use of MCE Products

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

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

Biological Activity

Description

All p38 MAPK Isoforms :

In Vitro

Oxidative StressMitochondrial FunctionOthers

Oxidative Stress

NSP-116 (10 μM; 1 h) inhibits UV-A or blue light LED-induced ROS production in HCE-T cells^[1].
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].

Mitochondrial Function

NSP-116 (10 μM; 1 h) protects the mitochondrial membrane potential of HCE-T cells exposed to UV-A or blue light LED^[1].

Others

NSP-116 (1-10 μM; 1 h) reduces cell death and maintains the viability of HCE-T cells exposed to UV-A or blue light LED^[1].
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.

Cell Viability Assay^[1]

Cell Line:

HCE-T
Concentration:

1, 3, 10 μM (NSP-116); 16.2 μM (Hoechst 33342); 1.5 μM (PI)
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)
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.

Western Blot Analysis^[1]

Cell Line:

HCE-T
Concentration:

10 μM
Incubation Time:

1 h
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.

Cell Viability Assay^[2]

Cell Line:

661 W cells
Concentration:

0.1, 1, 3, 10 μM
Incubation Time:

1 h
Result:

Inhibited the reduction in cell viability at 3 and 10 μM.

Parmacokinetics

Species	Dose	Route	C_max	T_max
Rat^[2]	25 mg/kg	p.o.	7.5 μg/mL	0.5 h
Rat^[2]	50 mg/kg	p.o.	15.3 μg/mL	0.5 h
Rat^[2]	100 mg/kg	p.o.	36.2 μg/mL	0.5 h
Rat^[2]	300 mg/kg	p.o.	112.8 μg/mL	1 h

In Vivo

ApoptosisOthers

Apoptosis

Topical administration of eye drops containing NSP-116 (10 μM; eye drops; twice daily; 10 days) ameliorates blue light LED-induced corneal epithelial cell apoptosis in mice, significantly reducing TUNEL-positive cells in the whole cornea to 2.5 cells per 1000 μm of corneal arc^[1].

Others

NSP-116 (10-30 mg/kg; p.o.; single administration; 30 min before light exposure) shows a protective effect against light-induced retinal damage in mice^[2].

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

Animal Model:

ddY mice (male, 7 weeks old)^[1]
Dosage:

10 μM
Administration:

Eye drops; twice daily; 10 days
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.

Animal Model:

ddY mice (eight-week-old, male)^[2]
Dosage:

10 or 30 mg/kg
Administration:

p.o.; single dose; 30 min before light exposure
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.

Related Protocols :

Chemical Information

CAS No. 1643925-08-9
Molecular Weight 285.34
Formula C₁₅H₁₉N₅O
SMILES

O=C(C)N1CCN(CC1)C2=CC=C(C(N3C=NC=C3)=C2)N
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]. Ishida K, et al. Free-Radical Scavenger NSP-116 Protects the Corneal Epithelium against UV-A and Blue LED Light Exposure. Biological & pharmaceutical bulletin. 2021;44(7):937-946.

[2]. Izawa H, et al. Protective effects of NSP-116, a novel imidazolyl aniline derivative, against light-induced retinal damage in vitro and in vivo. Free radical biology & medicine. 2016 Jul;96:304-12.

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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.

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

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NSP-116

All p38 MAPK Isoforms