FK 888

Catalog #: 2400
1 Citation Datasheet / COA / SDS

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FK 888 | CAS No. 138449-07-7 | NK1 Receptor Antagonists

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Description: High affinity NK1 antagonist

Chemical Name: (4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide

Purity: ≥98%

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Product Details

Citations (1)

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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

FK 888 is a selective, high affinity tachykinin NK₁ receptor antagonist (K_i = 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:

Sold with the permission of Astellas Pharma Inc.

Background References

Pharmacological profile of a high affinity dipeptide NK₁ receptor antagonist.
Fujii et al.
Br.J.Pharmacol., 1992;107:785
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
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

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Citation for FK 888

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

1 Citation: Showing 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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