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 (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.
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Shiga-Y51 Related Classifications
HY-D3429 Related Classifications
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