PTO-41
PTO-41 is a blood-brain barrier-permeable near-infrared fluorescent probe that targets β-amyloid oligomers (Aβ Oligomers, AβOs) with a Kd of 349 nM. PTO-41 exhibits low cytotoxicity, high sensitivity to β-amyloid oligomers in in vitro phantom imaging, and can be rapidly cleared from the brain. PTO-41 is applicable to the research of Alzheimer's disease (Ex/Em = 538 nM/680 nM).
For research use only. We do not sell to patients.
- CAS No.: 2408913-88-0
- Formula: C27H30BF2NO3
- Molecular Weight:465.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
In Vitro
PTO-41 (25 μM) selectively binds to Aβ42 oligomers in a brain-relevant biological environment, producing a significantly higher near-infrared fluorescence signal than with Aβ42 monomers or aggregates[1].
PTO-41 (0.1-10 μM; 24 h) shows negligible cytotoxicity towards SH-SY5Y human neuronal cells at concentrations up to 10 μM after 24 h incubation[1].
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:SH-SY5Y human neuronal cells
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Concentration:0.1, 1 and 10 μM
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Incubation Time:24 h
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Result:Exhibited negligible cytotoxicity, with cell viability remaining above 85% at all tested concentrations.
In Vivo
PTO-41 (intravenous injection) exhibits efficient blood-brain barrier penetration and rapid brain clearance in healthy ICR mice, with an initial brain uptake of 9.04 % ID/g at 2 min post-injection and a clearance rate of 5.0[1].
Guide (The following is our recommended experimental protocol. This protocol serves only as a reference guide, and specific operations should be adjusted according to your actual needs).
1. Preparation of PTO-41 Stock Solution
Weigh PTO-41 and dissolve it in DMSO to prepare a 25.0 μM stock solution. Store the solution at -20℃ away from light.
2. Fluorescence Binding Assay for Aβ Species
2.1 Dilute PTO-41 with PBS (pH 7.4) to a final concentration of 500 nM in a quartz cuvette.
2.2 Add pre-prepared Aβ42 monomers/oligomers/aggregates (final concentration 1.5 μM, i.e., probe:Aβ ≈ 1:3).
2.3 Mix well and incubate at room temperature for an appropriate period of time (usually several minutes until equilibrium is reached).
2.4 Measure fluorescence: Ex = 570 nm, Em scan = 600-800 nm (record the intensity at 680 nm).
2.5 Use PTO-41/PBS without Aβ as the blank for calibration.
3. In Vivo NIR Fluorescence Imaging in Mice
3.1 Reagent Preparation (Injection Solution):
Solvent system: 15% DMSO + 15% Cremophor EL + 70% PBS
The final concentration of PTO-41 is calculated based on 4 mg/kg body weight (100 μL is typically used for mice)
Prepare immediately before use, shake well and let stand for 20 min to ensure stable dissolution
3.2 Animal Imaging
3.2.1 Use 4-month-old female APP/PS1 transgenic mice and age-matched WT control mice (n=3-4).
3.2.2 Shave the head hair before the operation to reduce background interference.
3.2.3 Inject 100 μL of PTO-41 solution via tail vein.
3.2.4 Image acquisition using the IVIS Spectrum system:
Ex = 570 nm / Em = 680 nm
Time points for acquisition: before injection, 30, 60, 120, 240, 360 min
Draw ROIs on the brain in the software (Living Image 4.2.1) for quantitative analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:APP/PS1 transgenic mice (female, 4-month-old); wild-type mice (female, 4-month-old, age-matched control)[1]
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Dosage:4 mg/kg
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Administration:i.v.; single bolus injection
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Result:Reached maximum fluorescence intensity in the brain at 30 min post-injection.
Produced a near-infrared fluorescence (NIRF) signal ratio of 1.30 between APP/PS1 and wild-type mouse brains at 30 min post-injection.
Showed faster brain clearance than the reference probe PTO-29.
Chemical Information
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CAS No. 2408913-88-0
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Molecular Weight 465.34
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Formula C27H30BF2NO3
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SMILES
CCC1=CC=C(C=C1)C2=C(O[B-](F)([O+]=C2C3CC3)F)/C=C/C=C/C4=CC=C(C=C4)N(CCO)C
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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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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Amyloid: Congo Red Amyloid Staining
Congo red amyloid staining is a histochemical method used to detect extracellular amyloid deposits in tissue sections based on the affinity of Congo red dye for β-pleated sheet-rich protein aggregates. When bound to amyloid, Congo red produces characteristic apple-green birefringence under polarized light microscopy, which is widely regarded as a diagnostic feature of amyloid deposition in histopathology. The diagnostic principle relies on the combination of dye binding (congophilia) and optical anisotropy under polarized illumination, which distinguishes amyloid from most non-amyloid eosinophilic extracellular deposits in routine histological evaluation. Amyloid identification by Congo red staining remains a cornerstone in diagnostic pathology despite the availability of adjunct methods such as immunohistochemistry and mass spectrometry, particularly because of its ability to localize deposits directly within tissue architecture. The specificity of Congo red-positive deposits is incre
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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.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)