eNOS activator-1
eNOS activator-1 is an orally active, blood-brain barrier permeable endothelial nitric oxide synthase (eNOS) activator. eNOS activator-1 upregulates eNOS mRNA expression, enhances endogenous NO biosynthesis, and activates the eNOS signaling pathway to maintain blood-brain barrier integrity. eNOS activator-1 upregulates the protein expression levels of PI3K, AKT, p-PI3K, and p-AKT. eNOS activator-1 reduces oxidative stress levels by decreasing lipid peroxidation and restoring antioxidant enzyme activities. eNOS activator-1 upregulates the expression of tight junction proteins ZO-1 and occludin, increases Cav-1 expression, and inhibits MMP-9-mediated blood-brain barrier disruption. eNOS activator-1 can be used in the research of ischemic stroke.
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- Formule: C14H15NO6
- Masse moléculaire:293.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
eNOS |
PI3K |
Akt |
MMP-9 |
ZO-1 |
Cav-1 |
In Vitro
eNOS activator-1 (1.8-60 μM; 24 h) shows no detectable cytotoxicity in primary rat neuronal cells at concentrations as high as 60 μM[1].
eNOS activator-1 (50 μg/mL; 18 h at 25 °C) demonstrates excellent predicted passive blood-brain barrier permeability in the in vitro PAMPA assay[1].
eNOS activator-1 (0.9-30 μM) exerts strong and consistent neuroprotective activity against oxygen-glucose deprivation/reperfusion injury in primary rat cortical neurons[1].
eNOS activator-1 (0.005 mM; 1-10 h) releases a stable, low concentration of NO over a 10 hour in vitro incubation[1].
eNOS activator-1 (compound 10) exerts an in vitro blood-brain barrier protective effect in primary rat neuronal OGD/R cultures that is fully dependent on eNOS activation, which regulates downstream Cav-1 and MMP-9 signaling[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat primary neuronal cells
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Concentration:1.8-60 μM
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Incubation Time:24 h
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Result:Show no detectable cytotoxicity at concentrations up to 60 μM, with full retention of cell viability across the tested concentration range.
In Vivo
eNOS activator-1 (20-40 mg/kg; p.o.; single pretreatment 2 hours before MCAO then once daily; 6 consecutive days after surgery) exerts potent neuroprotective, anti-inflammatory, antioxidant, and BBB-preserving effects in the rat MCAO/R ischemic stroke model, reducing infarct volume to as low as 24.1% at the 40 mg/kg dose[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KM mice (male, 18-22 g, 22 days old)[1]
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Dosage:200 mg/kg; 400 mg/kg
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Administration:p.o.; daily; 7 consecutive days
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Result:Showed no acute neurological toxicities including tremor, convulsion, or death over the 7-day observation period.
Exhibited no difference in average body weight compared to the control group.
Demonstrated good tolerance at a daily dose of 400 mg/kg with a total accumulated dosage of 2.8 g/kg.
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Animal Model:Sprague-Dawley rats (male, 200-220 g)[1]
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Dosage:20 mg/kg; 40 mg/kg
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Administration:p.o.; single pretreatment 2 hours before MCAO then once daily; 6 consecutive days after surgery
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Result:Reduced infarct volume to 29.0% at the 20 mg/kg dose.
Reduced infarct volume to 24.1% at the 40 mg/kg dose.
Alleviated histopathological neuronal damage and restored normal neuronal and capillary morphology.
Dose-dependently reduced IL-6 levels and restored reduced IL-10 levels.
Suppressed activation of Iba-1+ microglia and GFAP+ astrocytes, decreased M1 (CD86+) microglia and increased M2 (CD206+) microglia polarization.
Reversed the MCAO/R-induced increase in MDA and decrease in SOD levels.
Upregulated expression of PI3K, AKT, p-PI3K, and p-AKT proteins.
Reduced Evans blue extravasation to preserve BBB integrity, upregulated expression of tight junction proteins ZO-1 and occludin, increased Cav-1 expression, decreased MMP-9 levels.
Significantly elevated eNOS mRNA expression at the 40 mg/kg dose.
Chemical Information
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Masse moléculaire 293.27
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Formule C14H15NO6
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SMILES
O=[N+]([O-])OCCOC1=CC=C2C(/C(OC2=C1)=C/CCC)=O
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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)
eNOS activator-1 Related Classifications
HY-189214 Related Classifications
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