A partial 5-HT4 agonist
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PF-04995274

Item No. 28776

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
tetrahydro-4-[[4-[[[4-[[(3R)-tetrahydro-3-furanyl]oxy]-1,2-benzisoxazol-3-yl]oxy]methyl]-1-piperidinyl]methyl]-2H-pyran-4-ol
CAS Number
1331782-27-4
Molecular Formula
C23H32N2O6
Formula Weight
432.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 30 mg/mlDMF: 20 mg/mlDMF:PBS (pH 7.2) (1:4): 0.25 mg/ml
SMILES
OC1(CCOCC1)CN(CC2)CCC2COC3=NOC4=CC=CC(O[C@H]5COCC5)=C43
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
InChi Key
WLLOFQROROXOMO-GOSISDBHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $38

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    5 mg

    $110

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    10 mg

    $202

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    25 mg

    $454

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    Product 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).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Brodney, M.A., Johnson, D.E., Sawant-Basak, A., et al. Identification of multiple 5‑HT4 partial agonist clinical candidates for the treatment of alzheimer’s disease. J. Med. Chem. 55(21), 9240-9254 (2012).