L-733,060 hydrochloride

Name: L-733,060 hydrochloride
Brand: Tocris Bioscience
SKU: 1145

Tocris Bioscience, part of Bio-Techne | Catalog # 1145

Citations (31)

COA / SDS

Potent NK1 antagonist

Key Product Details

Description:	Potent NK₁ antagonist
Chemical Name:	(2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
Purity:	≥99% (HPLC)
Molecular Weight:	439.83

View Full Technical Details for L-733,060 hydrochloride

Technical Data
Citations

Biological Activity for L-733,060 hydrochloride

L-733,060 hydrochloride is a potent NK₁ antagonist (K_i values are 0.08, 0.2 and 93.13 nM for gerbil, human and rat receptors, respectively). Produces anxiolytic-like effects in the gerbil elevated plus-maze. Exhibits antitumor activity in vitro. Also decreases HER2 activity and tumor growth in mice bearing HER2⁺ or EGFR⁺ breast tumors. Orally bioavailable and brain penetrant.

Licensing Information

Sold with the permission of Merck, Sharpe and Dohme Ltd.

Technical Data for L-733,060 hydrochloride

M. Wt	439.83
Formula	C₂₀H₁₉F₆NO.HCl
Storage	Store at RT
Purity	≥99% (HPLC)
CAS Number	148687-76-7
PubChem ID	11957600
InChi Key	DYEUTIUITGHIEO-APTPAJQOSA-N
Smiles	Cl[H].FC(F)(F)C1=CC(=CC(CO[C@H]2CCCN[C@H]2C2=CC=CC=C2)=C1)C(F)(F)F

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 for L-733,060 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	water	21.99	50 with gentle warming

Preparing Stock Solutions for L-733,060 hydrochloride

The following data is based on the product molecular weight 439.83.

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	4.55 mL	22.74 mL	45.47 mL
2.5 mM	0.91 mL	4.55 mL	9.09 mL
5 mM	0.45 mL	2.27 mL	4.55 mL
25 mM	0.09 mL	0.45 mL	0.91 mL

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References for L-733,060 hydrochloride

References are publications that support the biological activity of the product.

Garcia-Recio Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer. Cancer Res. 2013 PMID: 24030979
Seabrook L-733,060, a novel tachykinin NK₁ receptor antagonist; effects in [Ca²⁺]_i mobilisation, cardiovascular and dural extravasation assays. Eur.J.Pharmacol. 1996 PMID: 8982729
Varty The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 2002 PMID: 12225694
Kramer Distinct mechanism for antidepressant blockade of central substance P receptors. Science 1998 PMID: 9733503