L-733,060 hydrochloride

Key Product Details

Product Description

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.

Product Specifications for L-733,060 hydrochloride

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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

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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

Calculators

Background References

References are publications that support the biological activity of the product. See our Citations tab to view 37 publications citing the usage of this 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

Product Documents for L-733,060 hydrochloride