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    PF-06256142
    PF-06256142

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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 #: V4441
    CAS #: 1609583-14-3 (rotation +)Purity ≥98%

    Description: PF-06256142 is a novel, potent and selective orthosteric agonist of the D1 receptor with D1 EC50 of 30 nM and D1 binding Ki of 12 nM. It has reduced receptor desensitization relative to dopamine and other catechol-containing agonists. The discovery of D1 subtype-selective agonists with drug-like properties has been an enduring challenge for the greater part of 40 years. All known D1-selective agonists are catecholamines that bring about receptor desensitization and undergo rapid metabolism, thus limiting their utility as a therapeutic for chronic illness such as schizophrenia and Parkinson's disease. Our high-throughput screening efforts on D1 yielded a single non-catecholamine hit PF-4211 (6) that was developed into a series of potent D1 receptor agonist leads with high oral bioavailability and CNS penetration. An important structural feature of this series is the locked biaryl ring system resulting in atropisomerism. 

    References: J Med Chem. 2018 Nov 15.

    Related CAS: 1609583-15-4 (rotation -); 1609580-97-3 (racemic)  

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    PF-06256142

    Name: PF-06256142
    CAS#: 1609583-14-3 (rotation +)
    Chemical Formula: C21H16N4O2
    Exact Mass: 356.1273
    Molecular Weight: 356.385
    Elemental Analysis: C, 70.77; H, 4.53; N, 15.72; O, 8.98 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: PF-06256142; PF 06256142; PF06256142
    IUPAC/Chemical Name: (+)-4-(3-Methyl-4-(6-methylimidazo[1,2-a]pyrazin-5-yl)phenoxy)furo[3,2-c]-pyridine
    InChi Key: HWAIAGZSWHOLLK-UHFFFAOYSA-N
    InChi Code: InChI=1S/C21H16N4O2/c1-13-11-15(27-21-17-6-10-26-18(17)5-7-23-21)3-4-16(13)20-14(2)24-12-19-22-8-9-25(19)20/h3-12H,1-2H3
    SMILES Code: CC1=CC(OC2=NC=CC3=C2C=CO3)=CC=C1C4=C(N=CC5=NC=CN45)C


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