2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. PF-03246799

PF-03246799 (PF-3246799) 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.

For research use only. We do not sell to patients.

PF-03246799 Chemical Structure

PF-03246799 Chemical Structure

CAS No. : 1065110-62-4

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PF-03246799 Related Antibodies

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Description

PF-03246799 (PF-3246799) 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[1].

IC50 & Target[1]

5-HT2C Receptor

190 nM (EC50)

5-HT2C Receptor

160 nM (Ki)

Cellular Effect
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]
Molecular Weight

239.32

Formula

C15H17N3
CAS No.
SMILES

C12=NC(CC3=CC=CC=C3)=NC=C1CCNCC2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-03246799 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-032467991065110-62-4PF03246799PF 032467995-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptor5-HT2C receptorstress urinary incontinenceInhibitorinhibitorinhibit

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