L 760735

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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)
Citations (1)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

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

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.