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    PF-4840154
    PF-4840154

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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 #: V4431
    CAS #: 1332708-14-1Purity ≥98%

    Description: PF-4840154 is a novel, potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. TrpA1 is an ion channel involved in nociceptive and inflammatory pain. It is implicated in the detection of chemical irritants through covalent binding to a cysteine-rich intracellular region of the protein. PF-4840154  was identified from an HTS of the Pfizer chemical collection, a class of pyrimidines emerged as a non-reactive, non-covalently binding family of agonists of the rat and human TrpA1 channel. Given the issues identified with the reference agonist Mustard Oil (MO) in screening, a new, non-covalently binding agonist was optimized and proved to be a superior agent to MO for screening purposes. Compound 16a (PF-4840154) is a potent, selective agonist of the rat and human TrpA1 channel and elicited TrpA1-mediated nocifensive behaviour in mouse.

    References:  2011 Aug 15;21(16):4857-9. 


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    PF-4840154

    Name: PF-4840154
    CAS#: 1332708-14-1
    Chemical Formula: C26H38N6O2
    Exact Mass: 466.3056
    Molecular Weight: 466.63
    Elemental Analysis: C, 66.92; H, 8.21; N, 18.01; O, 6.86
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: PF-4840154; PF 4840154; PF4840154.
    IUPAC/Chemical Name: N-benzyl-4-(2-methylpropylamino)-2-[4-(oxan-3-ylmethyl)piperazin-1-yl] pyrimidine-5-carboxamide
    InChi Key: PPANZCQXFYBGHN-UHFFFAOYSA-N
    InChi Code: InChI=1S/C26H38N6O2/c1-20(2)15-27-24-23(25(33)28-16-21-7-4-3-5-8-21)17-29-26(30-24)32-12-10-31(11-13-32)18-22-9-6-14-34-19-22/h3-5,7-8,17,20,22H,6,9-16,18-19H2,1-2H3,(H,28,33)(H,27,29,30)
    SMILES Code: O=C(C1=CN=C(N2CCN(CC3COCCC3)CC2)N=C1NCC(C)C)NCC4=CC=CC=C4


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