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JNJ-39729209

Chemical Structure : JNJ-39729209

CAS No.: 1160606-90-5

JNJ-39729209 (JNJ39729209)

Catalog No.: PC-63414Not For Human Use, Lab Use Only.

JNJ-39729209 is a potent, selective TRPV1 antagonist with binding pKi of 7.8 and 7.9 for human and rat TRPV1, respectively.

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    Biological Activity

    JNJ-39729209 is a potent, selective TRPV1 antagonist with binding pKi of 7.8 and 7.9 for human and rat TRPV1, respectively.
    JNJ-39729209 inhibits proton activation of human and rat TRPV1 receptors with pIC50s of 7.9 and 8.5, respectively, also prevents TRPV1 activation by capsaicin and heat.
    JNJ-39729209 shows no agonist or antagonist activity forTRPV2, hTRPV4, or hTRPA1 at 10 uM.
    JNJ-39729209 blocks capsaicin-induced hypotension, inducesa mild hyperthermia and inhibits capsaicin-induced hypothermia in vivo.
    JNJ-39729209shows significant efficacy against carrageenan- and CFA-evoked thermal hyperalgesia and exhibits significant anti-tussive activity in a guinea-pig model of capsaicin-induced cough.

    Physicochemical Properties

    M.Wt 455.28
    Formula C19H11Cl2F3N4S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    2-(2,6-dichlorobenzyl)-N-(4-(trifluoromethyl)phenyl)thiazolo[5,4-d]pyrimidin-7-amine

    References

    1. Maher MP, et al. Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50.

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