L-733,060 hydrochloride
Tocris Bioscience, part of Bio-Techne | Catalog # 1145
Potent NK1 antagonist
Product Description
L-733,060 hydrochloride is a 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.Product Specifications
Molecular Weight
439.83
Formula
C20H19F6NO.HCl
Storage
Store at RT
Purity
≥98% (HPLC)
Chemical Name
(2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
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.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 8.8 | 20 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 all affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 11.37 mL | 56.84 mL | 113.68 mL |
| 1 mM | 2.27 mL | 11.37 mL | 22.74 mL |
| 2 mM | 1.14 mL | 5.68 mL | 11.37 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.27 mL |
Calculators
Molarity Calculator
Dilution Calculator
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Background References
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
Product Specific Notices for L-733,060 hydrochloride
For research use only
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