P3LC7LC-P
P3LC7LC-P is a blood-brain barrier-permeable BRAG2 ligand with a KD of 6.14 μM. P3LC7LC-P binds to BRAG2, thereby disrupting its interaction with the GluA2 subunit of the AMPA receptor and inhibiting glutamate-induced GluA2 endocytosis. P3LC7LC-P exerts neuroprotective effects in oxygen-glucose deprivation-induced and glutamate-induced neurotoxicity models, reduces ROS accumulation and inhibits apoptosis, and reduces cerebral infarct size in a rat model of transient middle cerebral artery occlusion. P3LC7LC-P can be used for the research of ischemic stroke.
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- Formule: C60H73N11O15S2
- Masse moléculaire:1252.42
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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
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Activité biologique
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Chemical Information
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Activité biologique
P3LC7LC-P (10-50 μM; 24 h) shows no cytotoxicity against HT22 cells, and the cell viability remains above 80% at all tested doses, even at concentrations up to 50 μM[1].
P3LC7LC-P (0.1-10 μM; 26 h) dose-dependently protects HT22 cells against glutamate-induced excitotoxicity, and restores cell viability to 91.92% at the concentration of 10 μM[1].
P3LC7LC-P (0.1-10 μM) protects primary cortical neurons from glutamate-induced excitotoxic injury, and restores cell viability to 71.11% at a concentration of 10 μM[1].
P3LC7LC-P (0.1-10 μM) protects primary cortical neurons against OGD/R-induced injury in a dose-dependent manner, and restores cell viability to 90.63% at 10 μM[1].
P3LC7LC-P (10 μM; 26 h) significantly reduces glutamate-induced ROS accumulation in HT22 cells[1].
P3LC7LC-P (10 μM; 26 h) significantly reduces glutamate-induced apoptosis of HT22 cells, decreasing the total apoptosis rate to 9.4%[1].
P3LC7LC-P (10 μM; 26 h) reduces the Bax/Bcl-2 ratio and the expression level of activated caspase-3[1].
P3LC7LC-P (10 μM; 3 h) significantly inhibits glutamate-induced GluA2 endocytosis in primary cortical neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HT22 cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:2 h (preincubation); 24 h (glutamate exposure)
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Result:Restored cell viability in a dose-dependent manner: viability reached 71.92% at 0.1 μM, 81.92% at 1 μM, and 91.92% at 10 μM.
Exceeded the protective efficacy of the positive control Tat-GluA2-3Y (68.72% viability at 10 μM).
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Cell Line:HT22 cells exposed to glutamate
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Concentration:10 μM
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Incubation Time:2 h (preincubation); 24 h (glutamate exposure)
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Result:Reduced ROS production by approximately 50% relative to the glutamate-only group.
Showed reduced DCFH-DA fluorescence intensity confirmed by flow cytometry quantification.
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Cell Line:HT22 cells exposed to glutamate
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Concentration:10 μM
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Incubation Time:2 h (preincubation); 24 h (glutamate exposure)
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Result:Reduced total HT22 cell apoptosis from 12.3% (glutamate alone) to 9.4%.
Showed efficacy comparable to Tat-GluA2-3Y (8.7% total apoptosis).
Confirmed reduced apoptotic nuclear condensation via Hoechst staining.
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Cell Line:HT22 cells exposed to glutamate
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Concentration:10 μM
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Incubation Time:2 h (preincubation); 24 h (glutamate exposure)
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Result:Significantly decreased the Bax/Bcl-2 ratio increased by glutamate alone.
Reduced cleaved caspase-3 activation induced by glutamate.
Showed efficacy comparable to Tat-GluA2-3Y.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) (male)[1]
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Dosage:8 mg/kg
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Administration:i.p.; single dose
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Result:Reduced cerebral infarct volume to 21.00%, compared to 31.51% in the tMCAO model group.
Chemical Information
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Masse moléculaire 1252.42
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Formule C60H73N11O15S2
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Sequence
{Tyr(4-Pentynoic acid)}-Lys-Cys-Gly-Tyr-Asn-Cys-Tyr-Gly (Disulfide bridge: Cys3-Cys7)
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Sequence Shortening
{Tyr(4-Pentynoic acid)}-KCGYNCYG (Disulfide bridge: Cys3-Cys7)
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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)
P3LC7LC-P Related Classifications
HY-P11848 Related Classifications
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