Lig4-4
Lig4-4 is an orally active and selective TREK-1 inhibitor, with an IC50 of 2.06 μM in rats. Lig4-4 improves neuronal viability, reduces cell apoptosis by upregulating cleaved-caspase-3 and downregulating Bcl-2, and decreases infarct volume. Lig4-4 exerts a neuroprotective effect against cerebral ischemia injury. Lig4-4 can be used in studies related to cerebral ischemia.
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- No. CAS: 3598-68-3
- Fòrmula: C9H7NO4
- Peso molecular:193.16
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
Caspase 3 |
Bcl-2 |
In Vitro
Lig4-4 potently and selectively inhibits the rat TREK-1 channel in CHO/TREK-1 cells, with an IC50 of 2.06 μM[1].
Lig4-4 (1-10 μM; 2 h OGD, 24 h reoxygenation) enhances the viability of in vitro cultured rat cortical neurons subjected to OGD/R injury and reduces the apoptosis level of in vitro cultured rat cortical neurons with OGD/R injury[1].
Lig4-4 (10 μM; 2 h OGD, 24 h reoxygenation) reverses the oxygen-glucose deprivation/reoxygenation (OGD/R)-induced upregulation of cleaved caspase-3 expression and downregulation of Bcl-2 expression in rat cortical neurons, without altering Bax expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:cultured rat cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation (OGD/R)
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Concentration:1, 3, 10 μM
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Incubation Time:2 h OGD; 24 h reoxygenation
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Result:Increased cell viability by 4.4% at 1 μM compared to the OGD/R group.
Increased cell viability by 5.5% at 3 μM compared to the OGD/R group.
Increased cell viability by 14.9% at 10 μM compared to the OGD/R group, raising viability to 73%.
Showed no effect on the viability of non-OGD/R-treated normal neurons.
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Cell Line:cultured rat cortical neurons exposed to OGD/R
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Concentration:1, 10 μM
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Incubation Time:2 h OGD; 24 h reoxygenation
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Result:Reduced neuronal apoptosis rate to 28.1% at 1 μM.
Reduced neuronal apoptosis rate to 24.7% at 10 μM.
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Cell Line:cultured rat cortical neurons exposed to OGD/R
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Concentration:10 μM (administered during OGD and reoxygenation)
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Incubation Time:2 h OGD; 24 h reoxygenation
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Result:Reduced OGD/R-induced upregulation of cleaved-caspase-3 expression.
Restored OGD/R-induced downregulation of Bcl-2 expression.
Showed no effect on Bax expression.
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, 270-290 g, middle cerebral artery occlusion model)[1]
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Dosage:10 mg/kg; 50 mg/kg
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Administration:p.o.; single dose
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Result:Reduced cerebral infarct volume from 38.8% to 28% at 50 mg/kg.
Did not produce a significant effect at 10 mg/kg.
Chemical Information
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No. CAS 3598-68-3
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Peso molecular 193.16
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Fòrmula C9H7NO4
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SMILES
O=C1OC(C[N+]([O-])=O)C2=C1C=CC=C2
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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)
Lig4-4 Related Classifications
HY-W269032 Related Classifications
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