A PDE2A inhibitor
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PF-05180999

Item No. 30374

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-(1-azetidinyl)-7-methyl-5-[1-methyl-5-[5-(trifluoromethyl)-2-pyridinyl]-1H-pyrazol-4-yl]-imidazo[5,1-f][1,2,4]triazine
CAS Number
1394033-54-5
Molecular Formula
C19H17F3N8
Formula Weight
414.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
λmax
258 nm
SMILES
CC1=NC(C2=C(C3=CC=C(C(F)(F)F)C=N3)N(C)N=C2)=C4N1N=CN=C4N5CCC5
InChi Code
InChI=1S/C19H17F3N8/c1-11-27-15(17-18(29-6-3-7-29)24-10-26-30(11)17)13-9-25-28(2)16(13)14-5-4-12(8-23-14)19(20,21)22/h4-5,8-10H,3,6-7H2,1-2H3
InChi Key
CLGCHUKGBICQTE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $41

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    5 mg

    $108

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    10 mg

    $196

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    Product Description

    PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor (IC50 = 1.6 nM).1 It is greater than 2000-fold selective for PDE2A over a panel of ten additional PDEs. PF-05180999 increases striatal, cortical, and hippocampal cGMP levels in mice in a dose-dependent manner. In vivo, it inhibits disruption of low frequency cortical δ oscillation induced by the NMDA antagonist MK-801 in rat brain when administered at a dose of 0.03 mg/kg. PF-05180999 (0.1 and 0.32 mg/kg) inhibits ketamine-induced increases in the number of working memory errors in a radial arm maze task in rats.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Helal, C.J., Arnold, E., Boyden, T., et al. Identification of a potent, highly selective, and brain penetrant phosphodiesterase 2A inhibitor clinical candidate. J. Med. Chem. 61(3), 1001-1018 (2018).