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Cat. No.: HY-W269032

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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.

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

CAS No.: 3598-68-3
Formula: C₉H₇NO₄
Molecular Weight:193.16

Storage:

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

Lig4-4 Chemical Structure

CAS No.: 3598-68-3

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

Caspase 3

Bcl-2

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

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.

Cell Viability Assay^[1]

Cell Line:

cultured rat cortical neurons exposed to oxygen-glucose deprivation followed by reoxygenation (OGD/R)
Concentration:

1, 3, 10 μM
Incubation Time:

2 h OGD; 24 h reoxygenation
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.

Apoptosis Analysis^[1]

Cell Line:

cultured rat cortical neurons exposed to OGD/R
Concentration:

1, 10 μM
Incubation Time:

2 h OGD; 24 h reoxygenation
Result:

Reduced neuronal apoptosis rate to 28.1% at 1 μM.
Reduced neuronal apoptosis rate to 24.7% at 10 μM.

Western Blot Analysis^[1]

Cell Line:

cultured rat cortical neurons exposed to OGD/R
Concentration:

10 μM (administered during OGD and reoxygenation)
Incubation Time:

2 h OGD; 24 h reoxygenation
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

Lig4-4 (50 mg/kg; p.o.; single dose) produces neuroprotective effects in rat MCAO models by reducing cerebral infarct volume to 28%^[1].

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

Animal Model:

Sprague-Dawley (male, 270-290 g, middle cerebral artery occlusion model)^[1]
Dosage:

10 mg/kg; 50 mg/kg
Administration:

p.o.; single dose
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

CAS No. 3598-68-3
Molecular Weight 193.16
Formula C₉H₇NO₄
SMILES

O=C1OC(C[N+]([O-])=O)C2=C1C=CC=C2
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]. Wang W, et al. Lig4-4 selectively inhibits TREK-1 and plays potent neuroprotective roles in vitro and in rat MCAO model. Neuroscience letters. 2018 Apr 03;671:93-98.

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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
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Lig4-4

All Caspase Isoforms

All Bcl-2 Family Isoforms