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PF-04995274

Catalog No. T16481   CAS 1331782-27-4

PF-04995274 is an effective, high-affinity, and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM). It also has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S).

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PF-04995274 Chemical Structure
PF-04995274, CAS 1331782-27-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 30.00
5 mg In stock $ 68.00
10 mg In stock $ 126.00
25 mg In stock $ 207.00
50 mg In stock $ 369.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 67.00
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Purity: 99.55%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description PF-04995274 is an effective, high-affinity, and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM). It also has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S).
In vitro PF-04995274 shows Ki values of 0.36 nM, 0.46 nM, 0.15 nM, 0.32 nM and 0.3nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S, respectively. PF-04995274 displays EC50 values of 0.47 nM, 0.36 nM, 0.37 nM, 0.26 nM, 0.59 nM, 0.65 nM and 0.62 nM for human 5-HT4A/4B/4D/4E and rat 5-HT4S/4L/4E, respectively [3].
In vivo PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment causes prophylactic efficacy by attenuating learned fear. It also decreasing stress-induced depressive-like behavior[1].
Molecular Weight 432.51
Formula C23H32N2O6
CAS No. 1331782-27-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (231.21 mM), sonification is recommended.

TargetMolReferences and Literature

1. Chen BK, et al. Prophylactic efficacy of 5-HT4R agonists against stress. Neuropsychopharmacology. 2019 Oct 10. 2. Grimwood S, et al. Translational receptor occupancy for the 5-HT4 partial agonist PF-04995274 in rats, non-human primates and healthy volunteers. Alzheimer’s Dement: J Alzheimer’s Assoc. 2011;7:S653. 3. Timothy Nicholas1, et al. Systems pharmacology modeling in neuroscience: Prediction and outcome of PF-04995274, a 5-HT4 partial agonist, in a clinical scopolamine impairment trial. Advances in Alzheimer's Disease. Vol.2 No.3(2013).

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library NO PAINS Compound Library CNS-Penetrant Compound Library Bioactive Compounds Library Max Anti-Parkinson's Disease Compound Library Anti-Alzheimer's Disease Compound Library Anti-Cancer Compound Library GPCR Compound Library Neuronal Signaling Compound Library

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Keywords

PF-04995274 1331782-27-4 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor 5-HT4 5-hydroxytryptamine Receptor behavior Alzheimer′s disease PF04995274 inhibit PF 04995274 Serotonin Receptor Stress-induced depressive-like inhibitor

 

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