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Referencia número: HY-P11848

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P3LC7LC-P

P3LC7LC-P is a blood-brain barrier-permeable BRAG2 ligand with a K_D 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.

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₆₀H₇₃N₁₁O₁₅S₂
Peso molecular:1252.42

Almacenamiento:

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

Síntesis personalizada de péptidos

P3LC7LC-P Chemical Structure

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Use of MCE Products

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

Actividad biológica
- Descripciòn
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
Help & FAQs
Classifications
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Actividad biológica

Descripciòn

Ver todos los productos específicos de isoformas iGluR :

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

HT22 cells
Concentration:

0.1, 1 and 10 μM
Incubation Time:

2 h (preincubation); 24 h (glutamate exposure)
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).

Others (Intracellular Reactive Oxygen Species Inhibition Assay)^[1]

Cell Line:

HT22 cells exposed to glutamate
Concentration:

10 μM
Incubation Time:

2 h (preincubation); 24 h (glutamate exposure)
Result:

Reduced ROS production by approximately 50% relative to the glutamate-only group.
Showed reduced DCFH-DA fluorescence intensity confirmed by flow cytometry quantification.

Apoptosis Analysis^[1]

Cell Line:

HT22 cells exposed to glutamate
Concentration:

10 μM
Incubation Time:

2 h (preincubation); 24 h (glutamate exposure)
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.

Western Blot Analysis^[1]

Cell Line:

HT22 cells exposed to glutamate
Concentration:

10 μM
Incubation Time:

2 h (preincubation); 24 h (glutamate exposure)
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.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞	Brain-to-Plasma Ratio
Rat^[1]	8 mg/kg	s.c.	0.452 h	1 h	6930 ng/mL	12100 ng·h/mL	12100 ng·h/mL	1.24 h	1.24 h	21.3 %
Rat^[1]	8 mg/kg	i.v.	0.589 h	0.0833 h	6290 ng/mL	3250 ng·h/mL	3250 ng·h/mL	0.683 h	0.691 h	/

In Vivo

P3LC7LC-P (8 mg/kg; i.p.; single administration) significantly reduces the cerebral infarction volume to 21.00% in a rat transient middle cerebral artery occlusion (tMCAO) model of ischemic stroke^[1].

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

Animal Model:

Sprague-Dawley (SD) (male)^[1]
Dosage:

8 mg/kg
Administration:

i.p.; single dose
Result:

Reduced cerebral infarct volume to 21.00%, compared to 31.51% in the tMCAO model group.

Chemical Information

Peso molecular 1252.42
Fòrmula C₆₀H₇₃N₁₁O₁₅S₂
Sequence

{Tyr(4-Pentynoic acid)}-Lys-Cys-Gly-Tyr-Asn-Cys-Tyr-Gly (Disulfide bridge: Cys3-Cys7)
Sequence Shortening

{Tyr(4-Pentynoic acid)}-KCGYNCYG (Disulfide bridge: Cys3-Cys7)
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Qin Y, et al. Stapled Peptides with Therapeutic Potential for Ischemic Stroke by Blocking the Endocytosis of GluA2 AMPAR. Journal of medicinal chemistry. 2026 Feb 12;69(3):3233-3251. [Content Brief]

Calculators

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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100 mg

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P3LC7LC-P

Ver todos los productos específicos de isoformas iGluR