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 No.: 945400-24-8
- Formule: C13H11N3OS
- Masse moléculaire:257.31
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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
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.
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 No. 945400-24-8
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Masse moléculaire 257.31
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Formule C13H11N3OS
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SMILES
OC1=CC=C2N=C(SC2=C1)C=3C=NC(=CC3)NC
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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]. 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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AZD-2184 Related Classifications
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