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Submit ReviewL 760735
Description: High affinity NK1 antagonist
Chemical Name: 5-[[(2R,3S)-2-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl-N,N-dimethyl-1H-1,2,3-triazole-4-methanamine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for L 760735
L 760735 is a 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 for L 760735
L 760735 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for L 760735
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for L 760735
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 18.36 | 30 | |
| DMSO | 30.6 | 50 |
Preparing Stock Solutions for L 760735
The following data is based on the product molecular weight 611.98. 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 |
|---|---|---|---|
| 0.5 mM | 3.27 mL | 16.34 mL | 32.68 mL |
| 2.5 mM | 0.65 mL | 3.27 mL | 6.54 mL |
| 5 mM | 0.33 mL | 1.63 mL | 3.27 mL |
| 25 mM | 0.07 mL | 0.33 mL | 0.65 mL |
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Product Datasheets for L 760735
References for L 760735
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for L 760735, please let us know.
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Keywords: L 760735, L 760735 supplier, L760735, NK1, antagonists, tachykinin, receptor, antagonist, neurokinin, 1, receptors, substance, P, Receptor, 4013, Tocris Bioscience
1 Citation for L 760735
Citations are publications that use Tocris products. Selected citations for L 760735 include:
Yin et al (2018) Crystal structure of the human NK1 tachykinin receptor. Proc.Natl.Acad.Sci.U.S.A. 115 13264 PMID: 30538204
Do you know of a great paper that uses L 760735 from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.