PF-03246799
PF-03246799 is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research.
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- CAS No.: 1065110-62-4
- Formule: C15H17N3
- Masse moléculaire:239.32
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
|
5-HT2C Receptor 190 nM (EC50) |
5-HT2C Receptor 160 nM (Ki) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
4.5 nM
Compound: 7b, PF-3246799
|
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
| NIH3T3 | EC50 |
190 nM
Compound: 7b, PF-3246799
|
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor expressed in Swiss mouse 3T3 cells with low expression increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
| NIH3T3 | EC50 |
4.5 nM
Compound: 7b, PF-3246799
|
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human 5HT2C receptor highly expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
| NIH3T3 | EC50 |
68 nM
Compound: 7b, PF-3246799
|
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
Agonist activity at human recombinant 5HT2A receptor expressed in Swiss mouse 3T3 cells increase of fluorescence based calcium mobilization by FLIPR assay
|
[PMID: 21195614] |
Chemical Information
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CAS No. 1065110-62-4
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Masse moléculaire 239.32
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Formule C15H17N3
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SMILES
C12=NC(CC3=CC=CC=C3)=NC=C1CCNCC2
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)