1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. PF-04995274

PF-04995274 

Cat. No.: HY-18137 Purity: 99.42%
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-04995274 Chemical Structure

PF-04995274 Chemical Structure

CAS No. : 1331782-27-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 76 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 250 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target

5-HT4 receptor[1][2][3]

In Vitro

PF-04995274 has 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. PF-04995274 has 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[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.
Molecular Weight

432.51

Formula

C₂₃H₃₂N₂O₆

CAS No.

1331782-27-4

SMILES

OC1(CN2CCC(COC3=NOC4=CC=CC(O[[email protected]]5COCC5)=C34)CC2)CCOCC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (231.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3121 mL 11.5604 mL 23.1209 mL
5 mM 0.4624 mL 2.3121 mL 4.6242 mL
10 mM 0.2312 mL 1.1560 mL 2.3121 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.78 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.42%

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Keywords:

PF-04995274PF04995274PF 049952745-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorStress-induceddepressive-likebehaviorAlzheimer′s disease 5-HT4Inhibitorinhibitorinhibit

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Product name:
PF-04995274
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HY-18137
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