PRX-03140
PRX-03140 is a selective, blood-brain-barrier permeable 5-HT4 receptor agonist with a Ki value of 110 nM against rat brain 5-HT4 receptor. PRX-03140 can increase cortical ACh and histamine levels. PRX-03140 can be used in the research of Alzheimer's disease.
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- No. CAS: 869493-21-0
- Fòrmula: C19H27N3O3S
- Peso molecular:377.50
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Ver todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
Descripciòn
IC50 & Target
Ki: 110 nM against rat brain 5-HT4 receptor[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
58 nM
Compound: PRX-03140
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Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay
|
[PMID: 26363507] |
| COS-7 | EC50 |
17 nM
Compound: PRX-03140
|
Agonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assay
Agonist activity at recombinant human 5HT4e receptor expressed in African green monkey COS7 cells assessed as cAMP level after 30 mins by HTRF assay
|
[PMID: 26363507] |
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 869493-21-0
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Peso molecular 377.50
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Fòrmula C19H27N3O3S
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SMILES
O=C(NCCCN1CCCCC1)C=2C(=O)N(C=3SC=CC3C2O)C(C)C
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Synonyms
VRX-03011 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocolo
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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.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)