Biological Activity
High affinity NK1 receptor antagonist (IC50 = 0.19 nM at human NK1 receptors). Selective (>300-fold) over h-NK2 and h-NK3 receptors. Exhibits anxiolytic and antidepressant-like effects. Orally active.
Compound Libraries
L 760735 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 611.98 |
| Formula | C26H28F7N5O2.HCl |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 188923-01-5 |
| PubChem ID | 9809076 |
| InChI Key | VZBKOBSSEVXFNF-QIRDZIKRSA-N |
| Smiles | FC(C=C3)=CC=[C@@]3[C@@H]1N(CC4=C(CN(C)C)NN=N4)CCO[C@@H]1O[C@H](C)C2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2.Cl |
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 | 30.6 | 50 | |
| water | 18.36 | 30 |
Preparing Stock Solutions
The following data is based on the product molecular weight 611.98. 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 | 1.63 mL | 8.17 mL | 16.34 mL |
| 5 mM | 0.33 mL | 1.63 mL | 3.27 mL |
| 10 mM | 0.16 mL | 0.82 mL | 1.63 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.33 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Harrison et al (2001) An orally active, water-soluble neurokinin-1 receptor antagonist suitable for both intravenous and oral clinical administration. J.Med.Chem. 44 4296 PMID: 11708932
Duffy et al (2002) Correlation of neurokinin (NK) 1 receptor occupancy in gerbil striatum with behavioral effects of NK1 antagonists. J.Pharmacol.Exp.Ther 301 536 PMID: 11961054
Keywords: L 760735, supplier, L760735, NK1, antagonists, tachykinin, receptor, antagonist, neurokinin, 1, receptors, substance, P, NK1, Receptor, NK1, Receptor, Tocris Bioscience
