PF-04781340
PF-04781340 is a potent and selective 5-HT2C receptor agonist, with an EC50 of 9 nM and a Ki of 3 nM, respectively. PF-04781340 exhibits weak partial agonist activity at the 5-HT2B receptor, with an EC50 of 1484 nM. PF-04781340 can be used in the research of obesity and psychiatric disorders.
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- CAS No.: 1648726-56-0
- Formule: C17H21N3
- Masse moléculaire:267.37
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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
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Help & FAQs
Voir tous les produits spécifiques à Isoform 5-HT Receptor
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Activité biologique
Description
IC50 & Target
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5-HT2C Receptor 9 nM (EC50) |
5-HT2B Receptor 1484 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
1484 nM
Compound: 7, PF-04781340
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Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
Agonist activity at human recombinant 5-HT2B receptor expressed in CHOK1 cells assessed as induction of Ca2+ mobilization after 1 hr by FLIPR assay
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[PMID: 25815155] |
In Vitro
PF-04781340 exhibits metabolic stability in human liver microsomes, with a CLint of 19 mL/min/mg[1].
PF-04781340 exhibits moderate passive permeability in RRCK cells, with a Papp value of 8 × 10-6 cm/s[1].
PF-04781340 exhibits a low P-gp efflux ratio of only 2.8 in MDCK-MDR1 cells, indicating a reduced risk of efflux from the central nervous system[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1648726-56-0
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Masse moléculaire 267.37
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Formule C17H21N3
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SMILES
CNC1=NC(CC2=CC=CC=C2)=CC3=C1CCNCC3
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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
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Fiche technique (268 KB)
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SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-04781340 Related Classifications
HY-116524 Related Classifications
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