Shiga-Y51
Shiga-Y51 is a molecular probe that can cross the blood-brain barrier and selectively bind Aβ oligomers. Shiga-Y51 can be imaged based on fluorine-19 nuclear magnetic resonance imaging (19F-MRI) technology. Shiga-Y51 exhibits extremely strong binding affinity for early to intermediate Aβ oligomers, while having almost no affinity for mature Aβ fibrils. Shiga-Y51 is a derivative of Curcumin (HY-N0005) and can inhibit the binding of Curcumin to Aβ oligomers with an IC50 of 34.61 µM. Shiga-Y51 can be used in research related to Alzheimer's disease.
For research use only. We do not sell to patients.
- CAS No.: 2700202-84-0
- Formula: C24H20F6O6
- Molecular Weight:518.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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
Shiga-Y51 (10 µM; 20 min) exhibits strong specific binding to Aβ oligomers and very weak binding to Aβ fibrils in an in vitro cell-free Aβ aggregate model[1].
Shiga-Y51 (0.01-30 µM; 30 min) competitively inhibits Curcumin binding to Aβ oligomers in a concentration-dependent manner in a cell-free Aβ oligomer model in vitro, with an IC50 of 34.61 µM.
Shiga-Y51 (50 µM) does not inhibit Aβ oligomer formation in the cell-free Aβ spherical oligomer model in vitro[1].
Shiga-Y51 (10 μM; 480 min) inhibits the increase in ThT fluorescence intensity during the early aggregation of Aβ peptides in a cell-free system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Shiga-Y51 (200 mg/kg; 0.5 mL/kg/min; i.v.; single administration; continuous infusion for 40 min) specifically targeted and accumulated in the Aβ oligomer regions highly expressed in the brain in the APP/PS1 double transgenic AD mouse model, thereby enabling in vivo detection and imaging of Aβ oligomers via 19F-MRI[1].
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 APP/PS1 double transgenic mice (aged 15-18 months); C57BL/6 background wild-type mice (aged 15-18 months)[1]
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Dosage:200 mg/kg
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Administration:i.v.; single dose; 30 min
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Result:Detected intense signals of Shiga-Y51 (m/z 517.1) and its fragment (m/z 229.0) in the cerebral cortex and hippocampus of APP/PS1 mice.
Detected only faint signals of Shiga-Y51 in the cerebral cortex of wild-type mice.
Showed a significant correlation between signal intensity of Shiga-Y51 in brain regions and the area of Aβ oligomer immunoreactivity in APP/PS1 mice.
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Animal Model:C57BL/6 background male wild-type mice (aged 6.5 months)[1]
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Dosage:200 mg/kg
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Administration:i.v.; single dose; 30 min
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Result:Detected Shiga-Y51 in brain extracts, confirming blood-brain barrier permeability.
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Animal Model:C57BL/6 background APP/PS1 double transgenic mice[2]
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Dosage:200 mg/kg
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Administration:i.v.; continuously infused at a rate of 0.5 mL/kg/min; single administration; for a duration of 40 minutes
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Result:Generated intense 19F-NMR signals, which subsequently declined in a time-dependent manner in the heads of both wild-type and APP/PS1 mice.
Chemical Information
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CAS No. 2700202-84-0
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Molecular Weight 518.40
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Formula C24H20F6O6
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SMILES
OC1=C(OC(F)(F)F)C=C(/C=C/C(C(C)(CC)C(/C=C/C2=CC=C(O)C(OC(F)(F)F)=C2)=O)=O)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Shiga-Y51 Related Classifications
HY-D3429 Related Classifications
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