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GR159897

Chemical Structure : GR159897

CAS No.: 158848-32-9

GR159897 (GR-159897)

Catalog No.: PC-70192Not For Human Use, Lab Use Only.

GR159897 is a potent non-peptide antagonist of tachykinin NK2 receptor with pKi of 9.5 in CHO cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    GR159897 is a potent non-peptide antagonist of tachykinin NK2 receptor with pKi of 9.5 in CHO cells.
    GR159897 competitively antagonises the contractions induced by GR64349 in guinea-pig trachea (pA2 8.7).
    GR159897 has negligible activity at human NK1 (pKi<5).
    GR159897 potently antagonises bronchoconstriction induced by GR6434 in the anaesthetised guinea-pig.
    GR159897 shows anxiolytic effects in animal models.

    Physicochemical Properties

    M.Wt 414.535
    Formula C23H27FN2O2S
    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

    5-Fluoro-3-[2-[4-methoxy-4-[[(R)-phenylsulfinyl]methyl]-1-piperidinyl]ethyl]-1H-indole

    References

    1. Beresford IJ, et al. Eur J Pharmacol. 1995 Jan 16;272(2-3):241-8.

    2. Walsh DM, et al. Psychopharmacology (Berl). 1995 Sep;121(2):186-91.

    3. Advenier C. Can J Physiol Pharmacol. 1995 Jul;73(7):878-84.

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