Biological Activity
Potent NK1 antagonist (Ki 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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 21.99 | 50mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 439.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.27 mL | 11.37 mL | 22.74 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.55 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.27 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Kramer et al (1998) Distinct mechanism for antidepressant blockade of central substance P receptors. Science 281 1640 PMID: 9733503
Seabrook et al (1996) L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays. Eur.J.Pharmacol. 317 129 PMID: 8982729
Varty et al (2002) The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 27 371 PMID: 12225694
Garcia-Recio et al (2013) Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer. Cancer Res. 73 6424 PMID: 24030979
Keywords: L-733,060 hydrochloride, supplier, Potent, NK1, antagonists, Tachykinin, Receptors, Neurokinin, L733060, NK1, Receptor, NK1, Receptor, Tocris Bioscience
