FK 888

Pricing Availability   Qty
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% (HPLC)
Citations (1)
Literature (2)

Biological Activity for FK 888

FK 888 is a 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.

Licensing Information

Sold with the permission of Astellas Pharma Inc.

Technical Data for FK 888

M. Wt 588.69
Formula C36H36N4O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 138449-07-7
PubChem ID 107967
Smiles O=C(N3[C@H]([C@](N[C@@H](CC5=CC(C=CC=C6)=C6C=C5)C(N(C)CC4=CC=CC=C4)=O)=O)C[C@@H](O)C3)C2=CN(C)C1=CC=CC=C12

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.

Solubility Data for FK 888

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 58.87 100
ethanol 58.87 100

Preparing Stock Solutions for FK 888

The following data is based on the product molecular weight 588.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.7 mL 8.49 mL 16.99 mL
5 mM 0.34 mL 1.7 mL 3.4 mL
10 mM 0.17 mL 0.85 mL 1.7 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

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References for FK 888

References are publications that support the biological activity of the product.

Fujii et al (1992) Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist. Br.J.Pharmacol. 107 785 PMID: 1282073

Murai et al (1993) Effects of an NK1 receptor antagonist, FK888, on constriction and plasma extravasation induced in guinea pig airway by neurokinins and capsaicin. Eur.J.Pharmacol. 236 7 PMID: 7686493

Aramori et al (1994) Subtype- and species-selectivity of a tachykinin receptor antagonist, FK888, for cloned rat and human tachykinin receptors. Eur.J.Pharmacol. 269 277 PMID: 7531648

If you know of a relevant reference for FK 888, please let us know.

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Keywords: FK 888, FK 888 supplier, High, affinity, NK1, receptor, antagonists, Tachykinin, Receptors, Neurokinin, FK888, Receptor, 2400, Tocris Bioscience

1 Citation for FK 888

Citations are publications that use Tocris products. Selected citations for FK 888 include:

Mondal et al (2013) Mechanism of ghrelin-induced gastric contractions in Suncus murinus (house musk shrew): involvement of intrinsic primary afferent neurons. PLoS One 8 e60365 PMID: 23565235

Do you know of a great paper that uses FK 888 from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Depression Poster

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.