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    Mavatrep
    Mavatrep

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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 #: V4517
    CAS #: 956274-94-5Purity ≥98%

    Description: Mavatrep (formerly known as JNJ-39439335) is a novel, orally bioavailable, potent and selective TRPV1 antagonist with Ki of 6.5 nM. It exhibits minimal effect on the enzymatic activity (IC50 > 25 μM) of CYP isoforms 3A4, 1A2, and 2D6. In a TRPV1 functional assay, using cells expressing recombinant human TRPV1 channels, Mavatrep antagonized capsaicin-induced Ca(2+) influx, with an IC50 value of 4.6 nM. In the complete Freund's adjuvant- and carrageenan-induced thermal hypersensitivity models, Mavatrep exhibited full efficacy, with ED80 values of 7.8 and 0.5 mg/kg, respectively, corresponding to plasma levels of 270.8 and 9.2 ng/mL, respectively. On the basis of its superior pharmacologic and safety profile, Mavatrep was selected for clinical development for the treatment of pain

    References:  2015 May 14;58(9):3859-74.


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    Mavatrep

    Name: Mavatrep
    CAS#: 956274-94-5
    Chemical Formula: C25H21F3N2O
    Exact Mass: 422.1606
    Molecular Weight: 422.4512
    Elemental Analysis: C, 71.08; H, 5.01; F, 13.49; N, 6.63; O, 3.79
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Technical InformationSynonym: JNJ-39439335; JNJ 39439335; JNJ39439335
    IUPAC/Chemical Name: (E)-2-(2-(2-(4-(trifluoromethyl)styryl)-1H-benzo[d]imidazol-6-yl)phenyl)propan-2-ol
    InChi Key: ORDHXXHTBUZRCN-NTEUORMPSA-N
    InChi Code: InChI=1S/C25H21F3N2O/c1-24(2,31)20-6-4-3-5-19(20)17-10-13-21-22(15-17)30-23(29-21)14-9-16-7-11-18(12-8-16)25(26,27)28/h3-15,31H,1-2H3,(H,29,30)/b14-9+
    SMILES Code: OC(C)(C)C1=CC=CC=C1C2=CC=C3N=C(/C=C/C4=CC=C(C(F)(F)F)C=C4)NC3=C2


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