A PDE4D inhibitor
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BPN14770

Item No. 34075

Technical Information
Formal Name
4-[[2-(3-chlorophenyl)-6-(trifluoromethyl)-4-pyridinyl]methyl]-benzeneacetic acid
CAS Number
1606974-33-7
Synonyms
  • Zatolmilast
Molecular Formula
C21H15ClF3NO2
Formula Weight
Purity
≥98%
Formulation
A solid
Methanol: Soluble
SMILES
O=C(CC1=CC=C(CC2=CC(C(F)(F)F)=NC(C3=CC(Cl)=CC=C3)=C2)C=C1)O
InChi Code
InChI=1S/C21H15ClF3NO2/c22-17-3-1-2-16(12-17)18-9-15(10-19(26-18)21(23,24)25)8-13-4-6-14(7-5-13)11-20(27)28/h1-7,9-10,12H,8,11H2,(H,27,28)
InChi Key
LTSUMTMGJHPGFX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BPN14770 is an inhibitor of phosphodiesterase 4D (PDE4D).1 It selectively inhibits dimeric PDE4DS129D and PDE4DS54D, which mimic the phosphorylated, activated forms of PDE4D, over wild-type dimeric PDE4D, dimeric PDE4DS133D, and monomeric PDE4D2 (IC50s = 7.8, 7.4, 1,018, 2,013, and 127 nM, respectively). BPN14770 (0.3-30 mg/kg) enhances novel object discrimination in mice. It decreases hyperarousal and increases social interaction time, indicating anxiolytic-like activity, nesting, and marble-burying behavior in the Fmr1-/- mouse model of fragile X syndrome when administered at a dose of 0.3 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gurney, M.E., Nugent, R.A., Mo, X., et alDesign and synthesis of selective phosphodiesterase 4D (PDE4D) allosteric inhibitors for the treatment of Fragile X Syndrome and other brain disorders. J. Med. Chem. 62(10), 4884-4901 (2019).

    2. Gurney, M.E., Cogram, P., Deacon, R.M., et alMultiple Behavior Phenotypes of the Fragile-X Syndrome Mouse Model Respond to Chronic Inhibition of Phosphodiesterase-4D (PDE4D). Sci. Rep. 7(1), 14653 (2017).