L57 acetate
Based on 1 Customer Validation
L57 acetate is a Low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 acetate exhibits high affinity to LRP1 with Ki of 45 nM. L57 acetate exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 acetate can be utilized as the carrier for CNS drug delivery.
For research use only. We do not sell to patients.
- Purity : 99.01%
- Formula: C120H175N31O27.xC2H4O2
- Molecular Weight:2483.87 (free base)
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Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
L57 (EC50-determining concentrations; 1 h) acetate selectively binds to recombinant human LRP1(CL4)-Fc with an EC50 of 45 nM in a plate ELISA assay[1].
Fluorescein-labeled L57 (3-30 μM; 4 h, 1 min) exhibits rapid, concentration-dependent, LRP1-mediated uptake in primary rat BMVECs and astrocytes, with significantly higher uptake efficiency than the reference peptide at matching concentrations, and shows limited uptake in LRP1-deficient PEA 10 cells[2].
Fluorescein-labeled L57 (3-30 μM; 4 h) shows excellent biocompatibility with no cytotoxicity observed in primary rat BMVECs or LRP1-deficient PEA 10 cells at concentrations up to 30 μM after 4 h of incubation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Primary rat brain microvascular endothelial cells (BMVECs), LRP1-deficient PEA 10 mouse embryonic fibroblasts
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Concentration:3 μM, 10 μM, 30 μM
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Incubation Time:4 h
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Result:Resulted in high cell viability in both BMVECs and PEA 10 cells, with metabolic activity comparable to vehicle control conditions at all tested concentrations.
In Vivo
L57 (i.v.; single dose) acetate results in modest brain delivery in male C57BL/6J mice, with a % input value of 0.042[1].
L57 acetate demonstrates significant blood-brain barrier permeability and high LRP1 binding affinity in healthy mice, supporting its potential as a CNS drug delivery vector[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Appearance Solid
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Molecular Weight 2483.87 (free base)
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Formula C120H175N31O27.xC2H4O2
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Color White to off-white
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Sequence
Thr-Trp-Pro-Lys-His-Phe-Asp-Lys-His-Thr-Phe-Tyr-Ser-Ile-Leu-Lys-Leu-Gly-Lys-His
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Sequence Shortening
TWPKHFDKHTFYSILKLGKH
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Protocols
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Sakamoto K, et al., A novel LRP1-binding peptide L57 that crosses the blood brain barrier. Biochem Biophys Rep. 2017 Aug 12;12:135-139. [Content Brief]
[2]. Rodrigues JP, et al. Efficient LRP1-Mediated Uptake and Low Cytotoxicity of Peptide L57 In Vitro Shows Its Promise as CNS Drug Delivery Vector. J Pharm Sci. 2021;110(2):824-832. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
L57 acetate Related Classifications
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