PF 04995274
- Product Name
- PF 04995274
- CAS No.
- 1331782-27-4
- Chemical Name
- PF 04995274
- Synonyms
- PF 04995274;PF-04995274 ，S0496;PF04995274;PF 04995274;PF-04995274 >=98% (HPLC);PF-04995274, 10 mM in DMSO;4-[[4-[[4-[(3R)-oxolan-3-yl]oxy-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxan-4-ol;(R)-4-((4-(((4-((Tetrahydrofuran-3-yl)oxy)benzo[d]isoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol;2H-Pyran-4-ol, tetrahydro-4-[[4-[[[4-[[(3R)-tetrahydro-3-furanyl]oxy]-1,2-benzisoxazol-3-yl]oxy]methyl]-1-piperidinyl]methyl]-;Inhibitor,5-HT4,5-hydroxytryptamine Receptor,behavior,Alzheimer′s disease,PF-04995274,inhibit,PF04995274,Serotonin Receptor,5-HT Receptor,Stress-induced,PF 04995274,depressive-like
- CBNumber
- CB42668576
- Molecular Formula
- C23H32N2O6
- Formula Weight
- 432.51
- MOL File
- 1331782-27-4.mol
PF 04995274 Property
- storage temp.
- Store at -20°C
- solubility
- DMSO:20.0(Max Conc. mg/mL);46.2(Max Conc. mM)
- form
- A crystalline solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 28776
- Product name
- PF-04995274
- Packaging
- 5mg
- Price
- $100
- Updated
- 2024/03/01
- Product number
- 28776
- Product name
- PF-04995274
- Packaging
- 25mg
- Price
- $412
- Updated
- 2024/03/01
- Product number
- 28776
- Product name
- PF-04995274
- Packaging
- 1mg
- Price
- $34
- Updated
- 2024/03/01
- Product number
- 28776
- Product name
- PF-04995274
- Packaging
- 10mg
- Price
- $183
- Updated
- 2024/03/01
- Product number
- CS-0007316
- Product name
- PF-04995274
- Purity
- 99.42%
- Packaging
- 5mg
- Price
- $80
- Updated
- 2021/12/16
PF 04995274 Chemical Properties,Usage,Production
Description
PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay). It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg.
Uses
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].
in vivo
PF-04995274 (3-10 mg/kg; intravenous injection; for 17 days; male 129S6/SvEv mice) treatment results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior[1].
| Animal Model: | Male 129S6/SvEv mice (7-8 weeks) treated with contextual fear conditioning (CFC) and forced swim test (FST)[1] |
| Dosage: | 3 mg/kg, 10 mg/kg |
| Administration: | Intravenous injection; for 17 days |
| Result: | Attenuated learned fear and decreased stress-induced depressive-like behavior. |
IC 50
5-HT4 Receptor
References
[1] Chen BK, et al. Prophylactic efficacy of 5-HT4R agonists against stress. Neuropsychopharmacology. 2019 Oct 10. DOI:10.1038/s41386-019-0540-3
[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).