L 760735

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Cat.No. 4013 - L 760735 | C26H28F7N5O2.HCl | CAS No. 188923-01-5
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)
Datasheet
Citations (1)
Reviews
Literature (6)

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 18.36 30
DMSO 30.6 50

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 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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References

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


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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


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Literature in this Area

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