Home Neuronal Signaling 5-HT Receptor agonist PF-04995274

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PF-04995274 5-HT Receptor agonist

Cat.No.S0496

PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. This compound is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
PF-04995274 5-HT Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 432.51

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Quality Control

Batch: S049601 DMSO]86 mg/mL]false]Ethanol]20 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (198.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

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Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 432.51 Formula

C23H32N2O6

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1331782-27-4 -- Storage of Stock Solutions

Synonyms PF-4995274 Smiles C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O

Mechanism of Action

Targets/IC50/Ki
human 5-HT4E
(Cell-free assay)
0.26 nM(EC50)
human 5-HT4B
(Cell-free assay)
0.36 nM(EC50)
human 5-HT4D
(Cell-free assay)
0.37 nM(EC50)
human 5-HT4A
(Cell-free assay)
0.47 nM(EC50)
rat 5-HT4S
(Cell-free assay)
0.59 nM(EC50)
rat 5-HT4E
(Cell-free assay)
0.62 nM(EC50)
rat 5-HT4L
(Cell-free assay)
0.65 nM(EC50)
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01193062 Completed
Healthy
Pfizer
 September 2010 Phase 1
NCT01173757 Completed
Healthy
Pfizer
 August 2010 Phase 1
NCT01091272 Completed
Healthy
Pfizer
 April 2010 Phase 1

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