FK 888
Tocris Bioscience, part of Bio-Techne | Catalog # 2400
High affinity NK1 antagonist
Product Description
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.Product Specifications
Molecular Weight
588.69
Formula
C36H36N4O4
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(4R)-4-Hydroxy-1-[(1-methyl-1H-indol-3-yl)carbonyl]-L-prolyl-N-methyl-3-(2-naphthalenyl)-N-(phenylmethyl)-L-alaninamide
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.
Solubility
| 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 all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.70 mL | 8.49 mL | 16.99 mL |
| 5 mM | 0.34 mL | 1.70 mL | 3.40 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.70 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Murai Effects of an NK1 receptor antagonist, FK888, on constriction and plasma extravasation induced in guinea pig airway by neurokinins and capsaicin. Eur.J.Pharmacol. 1993 PMID: 7686493
- Aramori Subtype- and species-selectivity of a tachykinin receptor antagonist, FK888, for cloned rat and human tachykinin receptors. Eur.J.Pharmacol. 1994 PMID: 7531648
- Fujii Pharmacological profile of a high affinity dipeptide NK1 receptor antagonist. Br.J.Pharmacol. 1992 PMID: 1282073
Product Specific Notices for FK 888
For research use only
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