Product Description: PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. 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), and 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). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease[1][2][3].
Applications: Neuroscience-Neurodegeneration
Formula: C23H32N2O6
References: [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).
CAS Number: 1331782-27-4
Molecular Weight: 432.51
Compound Purity: 99.95
Research Area: Neurological Disease
Solubility: DMSO : 100 mg/mL (ultrasonic)
Target: 5-HT Receptor
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