FK 888

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Cat.No. 2400 - FK 888 | C36H36N4O4 | CAS No. 138449-07-7
Description: High affinity NK1 receptor 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)
Datasheet
Citations (1)
Literature

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.

Licensing Information

Sold with the permission of Astellas Pharma Inc.

Compound Libraries

FK 888 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 588.69
Formula C36H36N4O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 138449-07-7
PubChem ID 107967
InChI Key BFNKQTIJVFGCKQ-PDJGWCFMSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 588.69. Batch specific molecular weights may vary from batch to batch due to solvent 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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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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


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