VHPKQHR
VHPKQHR is a peptide-based delivery enhancer that binds to VCAM-1. VHPKQHR enables intracellular internalization of relevant nanomaterials and facilitates the targeted delivery of miRNA inhibitors to inflamed endothelial cells and endothelial cells activated by disturbed flow. When conjugated with magnetic mesoporous silica nanoparticles, VHPKQHR achieves targeted accumulation at atherosclerotic plaque sites. When displayed on the surface of polyelectrolyte complex micelles, VHPKQHR enhances the relevant effects of anti-miR-92a in Apoe-/- mice. When conjugated with ultrasmall superparamagnetic iron oxide nanoparticles, VHPKQHR forms a contrast agent for T1-weighted magnetic resonance imaging. VHPKQHR can be used in research related to atherosclerosis, stenosis and rheumatoid arthritis.
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- CAS No.: 1174559-81-9
- Formule: C39H64N16O9
- Masse moléculaire:901.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[3]|
RDC Peptide |
In Vitro
VHPKQHR-displayed VCAM-1-targeting polyelectrolyte complex micelles (8 μg/mL; 30 min) selectively and efficiently deliver miRNA inhibitors to LPS-stimulated inflamed human aortic endothelial cells via VCAM-1 binding, with significantly higher uptake compared to nontargeting micelles[1].
UVHP modified with VHPKQHR peptide (5-200 µg/mL Fe; 12-24 h) has low cytotoxicity toward RAW264.7 macrophages and HFLS-RA cells at Fe concentrations up to 200 µg/mL[2].
UVHP modified with VHPKQHR peptide (25-200 µg/mL Fe; 24 h) selectively targets and is taken up at significantly higher levels by TNF-α-stimulated MAECs and HFLS-RA cells, which overexpress VCAM-1, compared to unstimulated cells[2].
The VHPKQHR peptide is successfully incorporated into Fe3O4@SiO2 nanoparticles to form FITC-VHP-Fe3O4@SiO2, as confirmed by UV-Vis and FTIR characterization[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
UVHP (250 µg Fe; i.v. via tail vein; single dose), modified with the VCAM-1-targeting VHPKQHR peptide, significantly increases T1-weighted MRI signal intensity and Fe accumulation in RA mouse knee joints, while showing no significant in vivo organ toxicity[2].
FITC-VHP-Fe3O4@SiO2 (modified with VHPKQHR peptide) (2.5 mg/kg; i.v.; single injection) specifically targets atherosclerotic plaques in ApoE-/- mice, reduces T2 relaxation time to enhance MRI contrast, and demonstrates low in vivo toxicity with no significant effects on organ function or morphology[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 background Apoe-/- (high-fat diet fed, partial carotid artery ligation-induced pathological vascular remodeling model)[1]
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Dosage:2 mg/kg miR-92a inhibitor
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Administration:i.v.; 3 total injections on days 5, 8, and 11 post-surgery
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Result:Reduced disturbed flow-induced carotid lesions by 89.2% compared to PBS-treated controls.
Left serum cholesterol levels and body weights unchanged.
Caused no significant tissue changes in major organs.
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Animal Model:C57BL/6 (2-month-old female, antigen-induced rheumatoid arthritis model)[2]
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Dosage:250 µg Fe
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Administration:i.v. via tail vein; single dose
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Result:Showed significantly higher T1-weighted MRI signal intensity of knee joints compared to UVHP-injected WT mice.
Showed significantly increased Fe content in knee joints compared to UVHP-injected WT mice, USPIO-injected WT mice, and USPIO-injected RA mice.
Demonstrated highest Fe accumulation in spleen, followed by liver, heart, lung, and kidney 24 hours post-injection.
Showed no significant morphological changes in major organs (heart, liver, spleen, lung, kidney) compared to PBS-injected RA mice 14 days post-injection.
Chemical Information
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CAS No. 1174559-81-9
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Masse moléculaire 901.03
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Formule C39H64N16O9
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SMILES
CC(C)[C@H](N)C(N[C@@H](CC1=CN=CN1)C(N2[C@@H](CCC2)C(N[C@@H](CCCCN)C(N[C@@H](CCC(N)=O)C(N[C@H](C(N[C@H](C(O)=O)CCCNC(N)=N)=O)CC3=CN=CN3)=O)=O)=O)=O)=O
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Sequence
Val-His-Pro-Lys-Gln-His-Arg
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Sequence Shortening
VHPKQHR
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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
[1]. Zhou Z, et al. Targeted polyelectrolyte complex micelles treat vascular complications in vivo. Proceedings of the National Academy of Sciences of the United States of America. 2021 Dec 14;118(50):e2114842118. [Content Brief]
[2]. Zhang C, et al. VHPKQHR Peptide Modified Ultrasmall Paramagnetic Iron Oxide Nanoparticles Targeting Rheumatoid Arthritis for T1-Weighted Magnetic Resonance Imaging. Front Bioeng Biotechnol. 2022 Feb 28;10:821256. [Content Brief]
[3]. Xu W, et al. VHPKQHR peptide modified magnetic mesoporous nanoparticles for MRI detection of atherosclerosis lesions. Artificial cells, nanomedicine, and biotechnology. 2019 Dec;47(1):2440-2448. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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