Biological Activity
Potent and highly selective competitive tachykinin NK1 receptor antagonist (IC50 = 2.3 nM).
Licensing Information
Sold with the permission of Merck Sharp and Dohme Ltd.
Compound Libraries
L-732,138 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 472.39 |
| Formula | C22H18F6N2O3 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 148451-96-1 |
| PubChem ID | 44396853 |
| InChI Key | BYYQYXVAWXAYQC-LJQANCHMSA-N |
| Smiles | O=C(N[C@@](CC2=CNC3=C2C=CC=C3)([H])C(OCC1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)=O)C |
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 | |||
| ethanol | 47.24 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 472.39. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.12 mL | 10.58 mL | 21.17 mL |
| 5 mM | 0.42 mL | 2.12 mL | 4.23 mL |
| 10 mM | 0.21 mL | 1.06 mL | 2.12 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Cascieri et al (1994) Characterization of the interaction of N-acyl-L-tryptophan benzyl ester neurokinin antagonists with the human neurokinin-1 receptor. J.Biol.Chem. 269 6587 PMID: 7509807
Kuo et al (1998) Lipopolysaccharide enhances neurogenic plasma exudation in guinea-pig airways. Br.J.Pharmacol. 125 711 PMID: 9831906
MacLeod et al (1993) N-Acyl-L-tryptophan benzyl esters: potent substance P receptor antagonists. J.Med.Chem. 36 2044 PMID: 8393115
MacLeod et al (1994) Identification of L-tryptophan derivatives with potent and selective antagonist activity at the NK1 receptor. J.Med.Chem. 37 1269 PMID: 7513763
Keywords: L-732,138, supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, L732138, merck, NK1, Receptor, NK1, Receptor, Tocris Bioscience
