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.
For research use only. We do not sell to patients.
- CAS No.: 1648726-56-0
- Formula: C17H21N3
- Molecular Weight:267.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All 5-HT Receptor Isoforms
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Biological Activity
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. Further protocols information, click here.
Chemical Information
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CAS No. 1648726-56-0
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Molecular Weight 267.37
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Formula C17H21N3
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SMILES
CNC1=NC(CC2=CC=CC=C2)=CC3=C1CCNCC3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)