PF-04995274

Catalog No.S0496 Synonyms: PF-4995274

For research use only.

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. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.

PF-04995274 Chemical Structure

CAS No. 1331782-27-4

Purity & Quality Control

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Biological Activity

Description 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. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
Targets
human 5-HT4E [1]
(Cell-free assay)
human 5-HT4B [1]
(Cell-free assay)
human 5-HT4D [1]
(Cell-free assay)
human 5-HT4A [1]
(Cell-free assay)
rat 5-HT4S [1]
(Cell-free assay)
Click to View More Targets
0.26 nM(EC50) 0.36 nM(EC50) 0.37 nM(EC50) 0.47 nM(EC50) 0.59 nM(EC50)

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 86 mg/mL
(198.83 mM)
Ethanol 20 mg/mL
(46.24 mM)
Water Insoluble

Chemical Information

Molecular Weight 432.51
Formula

C23H32N2O6

CAS No. 1331782-27-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CN(CCC1COC2=NOC3=C2C(=CC=C3)OC4CCOC4)CC5(CCOCC5)O

In vivo Formulation Calculator (Clear solution)

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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01193062 Completed Drug: PF-04995274 Healthy Pfizer September 2010 Phase 1
NCT01173757 Completed Drug: PF-04995274 Healthy Pfizer August 2010 Phase 1
NCT01091272 Completed Drug: PF-04995274 Healthy Pfizer April 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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