AZD-2184
AZD-2184 is a β-amyloid (Aβ(1-40)) fibril binder with blood-brain barrier permeability, exhibiting a Kd of 8.4 nM for hAβ(1-40). AZD-2184 binds to the same site as CPIB, shows low levels of non-specific binding to brain tissue, rapidly enters and clears from the brain tissue of normal rats, and binds reversibly to plaques in vivo. The radiolabeled form of AZD-2184 can serve as a PET ligand for the visualization of Aβ deposits. AZD-2184 is applicable to research related to Alzheimer's disease.
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- CAS. Nr.: 945400-24-8
- Formel: C13H11N3OS
- Molecular Weight:257.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
[3H]AZD2184 (13-100 nM) binds to hAβ(1-40) fibrils with high affinity at a Kd of 8.4 nM, and a secondary low-affinity binding site exists at higher concentrations[1].
AZD2184 (30 min) competively binds to Aβ(1-40) fibrils, with a Ki of 19.7 nM in displacing [3H]AZD2184, confirming its mutual displaceability with PIB[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Brain Concentration | T1/2 |
|---|---|---|---|---|
| Rat[1] | 0.25 μmol/Kg | i.v. | 1526 (at 2 min) nM | 6.8 min |
In Vivo
[3H]AZD-2184 (0.3 nmol/kg; intravenous injection; single 30-second infusion) binds reversibly to amyloid plaques in APP/PS1 mice, with a signal-to-background ratio twice that of [3H]PIB, and its labeling level decreases significantly at 40 minutes after administration[1].
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, approximately 18 months old)[1]
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Dosage:0.3 nmol/kg
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Administration:i.v.; single 30-second infusion
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Result:Labeled amyloid plaques with a distribution matching [3H]PIB, but with twice the signal-to-background ratio at 10 minutes post-administration.
Showed plaque labeling that declined significantly over time, with significantly lower levels observed at 40 and 80 minutes compared to 10 and 20 minutes post-injection (p = 0.0003).
Chemical Information
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CAS. Nr. 945400-24-8
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Molecular Weight 257.31
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Formel C13H11N3OS
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SMILES
OC1=CC=C2N=C(SC2=C1)C=3C=NC(=CC3)NC
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
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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.
Reinheit & Dokumentation
Verweise
[1]. Johnson AE, et al. AZD2184: a radioligand for sensitive detection of beta-amyloid deposits. Journal of neurochemistry. 2009 Mar;108(5):1177-86. [Content Brief]
[2]. Mattsson P, et al. β-Amyloid binding in elderly subjects with declining or stable episodic memory function measured with PET and [¹¹C]AZD2184. European journal of nuclear medicine and molecular imaging. 2015 Sep;42(10):1507-11. [Content Brief]
[3]. Murugan NA, et al. The Culprit Is in the Cave: The Core Sites Explain the Binding Profiles of Amyloid-Specific Tracers. The journal of physical chemistry letters. 2016 Sep 01;7(17):3313-21. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)