Catalog Number: 2400
Chemical Name: (4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide
Biological Activity
Selective, high affinity tachykinin NK1 receptor antagonist (Ki = 0.69 nM) that displays 320-fold selectivity for human over rat NK1 receptors. Inhibits substance P-induced contraction of isolated guinea pig trachea (IC50 = 32 nM) and inhibits substance P-induced airway constriction in vivo following i.v. and oral administration.
Technical Data
  • M.Wt:
    588.69
  • Formula:
    C36H36N4O4
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at -20°C
  • CAS No:
    138449-07-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold with the permission of Astellas Pharma Inc.
Background References
  1. Subtype- and species-selectivity of a tachykinin receptor antagonist, FK888, for cloned rat and human tachykinin receptors.
    Aramori et al.
    Eur.J.Pharmacol., 1994;269:277
  2. Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist.
    Fujii et al.
    Br.J.Pharmacol., 1992;107:785
  3. Effects of an NK1 receptor antagonist, FK888, on constriction and plasma extravasation induced in guinea pig airway by neurokinins and capsaicin.
    Murai et al.
    Eur.J.Pharmacol., 1993;236:7
Citations:

The citations listed below are publications that use Tocris products. Selected citations for FK 888 include:

1 Citations: Showing 1 - 1

  1. Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons.
    Authors: Mondal Et al.
    PLoS One 2013;8:e60365

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