Basic information Safety Supplier Related

PF 04995274

Basic information Safety Supplier Related

PF 04995274 Basic information

Product Name:
PF 04995274
Synonyms:
  • PF 04995274
  • 4-[[4-[[4-[(3R)-oxolan-3-yl]oxy-1,2-benzoxazol-3-yl]oxymethyl]piperidin-1-yl]methyl]oxan-4-ol
  • PF04995274;PF 04995274
  • 2H-Pyran-4-ol, tetrahydro-4-[[4-[[[4-[[(3R)-tetrahydro-3-furanyl]oxy]-1,2-benzisoxazol-3-yl]oxy]methyl]-1-piperidinyl]methyl]-
  • PF-04995274 >=98% (HPLC)
  • 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
  • (R)-4-((4-(((4-((Tetrahydrofuran-3-yl)oxy)benzo[d]isoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol
  • PF-04995274, 10 mM in DMSO
CAS:
1331782-27-4
MF:
C23H32N2O6
MW:
432.51
Mol File:
1331782-27-4.mol
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PF 04995274 Chemical Properties

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
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PF 04995274 Usage And Synthesis

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).

PF 04995274Supplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
Taizhou Tongxin Bio-Tech Co., Ltd
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0523-86818997 18652728585
Email
sales@allyrise.com
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Taizhou Ruixin Chemical Co., Ltd.
Tel
0576-89085261 15867635987
Email
jasonhu09@163.com
Shanghai EFE Biological Technology Co., Ltd.
Tel
021-65675885 18964387627
Email
info@efebio.com
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