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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% (HPLC)
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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 for FK 888
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
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