D-520
D-520 is a potent and brain-penetrant dopamine D2/D3 agonist (D2 EC50 = 4.73 nM, Ki = 41.8 nM; D3 EC50 = 2.18 nM, Ki = 0.35 nM). D-520 inhibits the formation of Aβ aggregates in vitro and promotes the disaggregation of both alpha-synuclein (α-syn) and Aβ aggregates. D-520 exhibits efficacious activity in animal models of Parkinson’s disease (PD). D-520 can be used for PD and PD with dementia (PDD) research[1][2].
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- CAS No.: 1619269-47-4
- Formule: C31H39N3O3
- Masse moléculaire:501.66
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
[2]|
D2 Receptor 4.73 nM (EC50) |
D3 Receptor 2.18 nM (EC50) |
D2L Receptor 41.8 nM (Ki) |
D3 Receptor 0.35 nM (Ki) |
In Vitro
D-520 (0.01-30 μM, 24 h) exhibits dose-dependent neuroprotective effects against 6-hydroxydopamine (6-OHDA) (HY-B1081)-induced toxicity in MN9D dopaminergic cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 1619269-47-4
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Masse moléculaire 501.66
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Formule C31H39N3O3
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SMILES
OC1=CC(C2=CC=C(N3CCN(CCN(CCC)[C@@H]4CC5=C(C(O)=CC=C5)CC4)CC3)C=C2)=CC=C1O
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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.
Protocole
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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.
Pureté et documentation
Références
[1]. Yedlapudi D, et al. Targeting alpha synuclein and amyloid beta by a multifunctional, brain-penetrant dopamine D2/D3 agonist D-520: Potential therapeutic application in Parkinson's disease with dementia. Sci Rep. 2019 Dec 23;9(1):19648. [Content Brief]
[2]. Modi G, et al. Multifunctional D2/D3 agonist D-520 with high in vivo efficacy: modulator of toxicity of alpha-synuclein aggregates. ACS Chem Neurosci. 2014 Aug 20;5(8):700-17. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)