| Name | PF-04995274 |
| 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 demonstrates prophylactic efficacy by reducing learned fear and decreasing stress-induced depressive-like behavior[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (9.25 mM), Sonication is recommended.
DMSO : 100 mg/mL (231.21 mM), Sonication is recommended.
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| Keywords | Stress-induced | Serotonin Receptor | PF-04995274 | PF04995274 | PF 04995274 | Inhibitor | inhibit | depressive-like | behavior | Alzheimer′s disease | 5-hydroxytryptamine Receptor | 5HTReceptor | 5-HT4 receptor | 5-HT4 | 5-HT Receptor | 5HT Receptor |
| Inhibitors Related | Alverine citrate | Sevoflurane | Dapoxetine hydrochloride | Cefaclor monohydrate | Clozapine N-Oxide | 1,8-Cineole | Dopamine hydrochloride | Cloperastine hydrochloride | Mianserin hydrochloride | Trazodone hydrochloride | Cinchonidine | Doxepin hydrochloride |
| Related Compound Libraries | Failed Clinical Trials Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Serotonin Receptor-Targeted Compound Library | Anti-Cancer Drug Library |
United States
