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    PF-05180999
    PF-05180999

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V4447
    CAS #: 1394033-54-5 Purity ≥98%

    Description: PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. PF-05180999 was identified as a preclinical candidate targeting cognitive impairment associated with schizophrenia. PF-05180999 demonstrated potent binding to PDE2A in brain tissue, dose responsive mouse brain cGMP increases, and reversal of N-methyl-d-aspartate (NMDA) antagonist-induced (MK-801, ketamine) effects in electrophysiology and working memory models in rats. Preclinical pharmacokinetics revealed unbound brain/unbound plasma levels approaching unity and good oral bioavailability resulting in an average concentration at steady state (Cav,ss) predicted human dose of 30 mg once daily (q.d.). Modeling of a modified release formulation suggested that 25 mg twice daily (b.i.d.) could maintain plasma levels of PF-05180999 at or above targeted efficacious plasma levels for 24 h, which became part of the human clinical plan.

    References: J Med Chem. 2018 Feb 8;61(3):1001-1018.


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    PF-05180999

    Name: PF-05180999
    CAS#: 1394033-54-5
    Chemical Formula: C19H17F3N8
    Exact Mass: 414.1528
    Molecular Weight: 414.3962
    Elemental Analysis: C, 55.07; H, 4.14; F, 13.75; N, 27.04
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: PF 5180999; PF999; PF-999; PF 999; PF05180999; PF-05180999; PF 5180999; PF5180999; PF-5180999;
    IUPAC/Chemical 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
    InChi Key: CLGCHUKGBICQTE-UHFFFAOYSA-N
    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
    SMILES Code: FC(C1=CN=C(C2=C(C3=C4C(N5CCC5)=NC=NN4C(C)=N3)C=NN2C)C=C1)(F)F


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