PF-04995274
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 525952

CAS#: 1331782-27-4

Description: PF-04995274 is a 5-HT4 receptor partial agonist. It is thought to act centrally as a pro-cognitive agent that is being developed for the treatment of Alzheimer's disease (AD).

Chemical Structure

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PF-04995274
CAS# 1331782-27-4
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525952
Name: PF-04995274
CAS#: 1331782-27-4
Chemical Formula: C23H32N2O6
Exact Mass: 432.23
Molecular Weight: 432.520
Elemental Analysis: C, 63.87; H, 7.46; N, 6.48; O, 22.19

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 650 Ready to ship
200mg USD 1050 Ready to ship
500mg USD 1950 Ready to ship
1g USD 3150 Ready to ship
2g USD 4950 Ready to ship
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Synonym: PF-04995274; PF 04995274; PF04995274; PF-4995274; PF 4995274; PF4995274.

IUPAC/Chemical Name: (R)-4-((4-(((4-(Tetrahydrofuran-3-yloxy)-1,2-benzisoxazol-3-yl)oxy)methyl)piperidin-1-yl)methyl)tetrahydro-2H-pyran-4-ol

InChi Key: WLLOFQROROXOMO-GOSISDBHSA-N

InChi Code: InChI=1S/C23H32N2O6/c26-23(7-12-27-13-8-23)16-25-9-4-17(5-10-25)14-29-22-21-19(30-18-6-11-28-15-18)2-1-3-20(21)31-24-22/h1-3,17-18,26H,4-16H2/t18-/m1/s1

SMILES Code: OC1(CN2CCC(COC3=NOC4=C3C(O[C@H]5COCC5)=CC=C4)CC2)CCOCC1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: PF-04995274 is a partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively.
In vitro activity: TBD
In vivo activity: Whether PF-04995274 can be prophylactic in male 129S6/SvEv mice was evaluated. Male 129S6/SvEv mice were injected with saline or PF-04995274 (3 or 10 mg/kg) (Fig. 4a). One week later, mice were administered 3-shock CFC (contextual fear conditioning). Both groups of mice exhibited comparable levels of freezing during CFC training (Fig. 4b). Five days later, mice were re-exposed to the training context. PF-04995274 at 10, but not 3 mg/kg, attenuated learned fear when compared with saline administration. Stress-induced anxiety-like behavior was next quantified. In the OF, all groups of mice traveled a comparable distance (Fig. 4h). In the EPM (elevated plus maze), all groups of mice spent comparable time in the open arms (Fig. 4i) and entered into the open arms a comparable number of times (Fig. 4j). In the NSF (novelty suppressed feeding) paradigm, all groups of mice approached the pellet in a comparable amount of time (Fig. 4k, l). Finally, all mice lost a comparable amount of weight during the NSF paradigm (Fig. 4m). In summary, these data indicate that a single injection of PF-04995274 results in prophylactic efficacy by attenuating learned fear and decreasing stress-induced depressive-like behavior. Reference: Neuropsychopharmacology. 2020 Feb;45(3):542-552. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6969048/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.0 46.20

Preparing Stock Solutions

The following data is based on the product molecular weight 432.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Chen BK, Mendez-David I, Luna VM, Faye C, Gardier AM, David DJ, Denny CA. Prophylactic efficacy of 5-HT4R agonists against stress. Neuropsychopharmacology. 2020 Feb;45(3):542-552. doi: 10.1038/s41386-019-0540-3. Epub 2019 Oct 10. PMID: 31600767; PMCID: PMC6969048.
In vitro protocol: TBD
In vivo protocol: 1. Chen BK, Mendez-David I, Luna VM, Faye C, Gardier AM, David DJ, Denny CA. Prophylactic efficacy of 5-HT4R agonists against stress. Neuropsychopharmacology. 2020 Feb;45(3):542-552. doi: 10.1038/s41386-019-0540-3. Epub 2019 Oct 10. PMID: 31600767; PMCID: PMC6969048.

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1: Nirogi R, Kandikere V, Bhyrapuneni G, Saralaya R, Ajjala DR, Aleti RR, Rasheed MA. In-vivo rat striatal 5-HT4 receptor occupancy using non-radiolabelled SB207145. J Pharm Pharmacol. 2013 May;65(5):704-12. doi: 10.1111/jphp.12030. Epub 2013 Jan 25. PubMed PMID: 23600388.