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Cat. No.: HY-P11771

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KS-487

KS-487 is a cyclic peptide targeting LRP1 that binds to cluster IV (CL4) domain of LRP1 and facilitates molecular delivery to brain tissue via receptor-mediated transcytosis (RMT). The EC₅₀ of KS-487 binding to human LRP1 (CL4) is 10.5 nM. Compared with Angiopep-2, KS-487 exhibits enhanced brain selectivity and can be used in studies related to brain-targeted delivery systems.

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

Formula: C₇₃H₁₁₁N₁₅O₂₂S₂
Molecular Weight:1614.88

Storage:

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

Custom Peptide Synthesis

KS-487 Chemical Structure

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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
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target^[2]

HLRP1

10.5 nM (EC₅₀)

In Vitro

KS-487 selectively binds to the human LRP1 cluster IV domain, with a binding EC₅₀ of 10.5 nM^[2].

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

In Vivo

ICG-KS-487 (37.5 pmol; s.c.; single dose) exhibits in vivo blood-brain barrier permeability comparable to ICG-Angiopep-2, with a higher brain-to-liver selectivity ratio of 0.0847 at 72 hours post-subcutaneous administration, and shows no observable toxicity in mice^[3].
KS-487 (i.v.; single dose) acts as an LRP1-targeting moiety to enhance nanoparticle accumulation in CT26 tumors, resulting in higher tumor retention of nanoparticles compared to non-targeted nanoparticles^[4].

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

Animal Model:

BALB/cCrSlc (female, 6 weeks old, average weight 18 g)^[3]
Dosage:

37.5 pmol
Administration:

s.c.; single dose
Result:

Showed comparable brain permeability to ICG-Angiopep-2 and increased brain selectivity.

Chemical Information

Molecular Weight 1614.88
Formula C₇₃H₁₁₁N₁₅O₂₂S₂
Sequence

Ac-Gly-Thr-Pro-Cys-Thr-Tyr-Lys-Tyr-{Nle}-Leu-Ala-Glu-{Nle}-Cys (disulfide bridge:Cys4-Cys14)
Sequence Shortening

Ac-GTPCTYKY-{Nle}-LAE-{Nle}-C (disulfide bridge:Cys4-Cys14)
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]. Sakamoto K, et al. Cyclic Peptides KS-133 and KS-487 Multifunctionalized Nanoparticles Enable Efficient Brain Targeting for Treating Schizophrenia. JACS Au. 2024 Aug 26;4(8):2811-2817. [Content Brief]

[2]. Sakamoto K, et al. Generation of KS-487 as a novel LRP1-binding cyclic peptide with higher affinity, higher stability and BBB permeability. Biochemistry and biophysics reports. 2022 Dec;32:101367.

[3]. Asukabe K, et al. A Next-Generation Brain-Targeting Peptide: KS-487 Rivals Angiopep-2 in BBB Penetration with Enhanced Selectivity. Bioconjugate chemistry. 2025 Oct 15;36(10):2124-2131.

[4]. Sakamoto K, et al. KS-133/KS-487 Nanoparticles Exhibit Potent Antitumor Effects through Synergistic LRP1 Targeting and VIPR2 Inhibition: Therapeutic Nanoarchitectonics for Solid Tumors. Advanced Therapeutics. 2024;7:2400278.

Calculators

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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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100 mg

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