PF-04995274

• UNSPSC 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].

• Target Antigen:

  5-HT Receptor

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;Neuronal Signaling

• Applications:

  Neuroscience-Neurodegeneration

• Field of Research:

  Neurological Disease

• Assay Protocol:

  https://www.medchemexpress.com/pf-04995274.html

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

  OC1(CN2CCC(COC3=NOC4=CC=CC(O[C@H]5COCC5)=C34)CC2)CCOCC1

• Molecular Weight:

  432.51

• References & Citations:

  [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).

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 1

• CAS Number:

  1331782-27-4