2. Antibody-Drug Conjugate/ADC Related Neuronal Signaling
  3. Radionuclide-Drug Conjugates (RDCs) Amyloid-β
  4. 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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AZD-2184

AZD-2184 Chemical Structure

CAS No. : 945400-24-8

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AZD-2184 Related Antibodies

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Description

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[1][2][3].

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.

AZD-2184 Related Antibodies
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

AZD-2184 (0.25 μmol/kg; intravenous injection; single slow bolus injection) rapidly penetrates into the brain tissue of normal rats. At 2 minutes after intravenous administration, the proportion of the compound in brain tissue reaches 1.0%, with a half-life of 6.8 minutes in the brain[1].
[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.

Animal Model: APP/PS1 (transgenic, approximately 18 months old)[1]
Dosage: 0.3 nmol/kg
Administration: i.v.; single 30-second infusion
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).
Molecular Weight

257.31

Formula

C13H11N3OS
CAS No.
SMILES

OC1=CC=C2N=C(SC2=C1)C=3C=NC(=CC3)NC
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AZD-2184 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AZD-2184945400-24-8AZD2184AZD 2184Radionuclide-Drug Conjugates (RDCs)Amyloid-ββ-amyloid peptideAβAbetaAlzheimer's diseaseAβ(17?42) protofibrils[11C]PIBmouse cortical sectionsrat brainPET ligandspostmortem human cortical sectionsblood-brain barrierβ-amyloid (Aβ(1-40)) fibrilAβ depositsInhibitorinhibitorinhibit

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