Catalog Number: 1145
Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
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.
Technical Data
  • M.Wt:
    439.83
  • Formula:
    C20H19F6NO.HCl
  • Solubility:
    Soluble to 50 mM in water with gentle warming
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    148687-76-7
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.
Additional Information
Licensing Caveats:
Sold with the permission of Merck, Sharpe and Dohme Ltd.
Background References
  1. Distinct mechanism for antidepressant blockade of central substance P receptors.
    Kramer et al.
    Science, 1998;281:1640
  2. The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists.
    Varty et al.
    Neuropsychopharmacology, 2002;27:371
  3. L-733,060, a novel tachykinin NK1 receptor antagonist; effects in [Ca2+]i mobilisation, cardiovascular and dural extravasation assays.
    Seabrook et al.
    Eur.J.Pharmacol., 1996;317:129
  4. Substance P autocrine signaling contributes to persistent HER2 activation that drives malignant progression and drug resistance in breast cancer.
    Garcia-Recio et al.
    Cancer Res., 2013;73:6424
Citations:

The citations listed below are publications that use Tocris products. Selected citations for L-733,060 hydrochloride include:

10 Citations: Showing 1 - 10
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  1. A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer.
    Authors: D'Amato Et al.
    Cancer Res 2015;75:4651
  2. The Transmodulation of HER2 and EGFR by Substance P in Breast Cancer Cells Requires c-Src and Metalloproteinase Activation.
    Authors: García-Recio Et al.
    PLoS One 2015;10:e0129661
  3. Substance P reduces TNF-α-induced apoptosis in human tenocytes through NK-1 receptor stimulation.
    Authors: Backman Et al.
    Mol Cancer Res 2014;48:1414
  4. TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis.
    Authors: Liu Et al.
    FASEB J 2013;27:3549
  5. Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells.
    Authors: Li Et al.
    Am J Physiol Regul Integr Comp Physiol 2013;11:294
  6. Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation.
    Authors: Nassini Et al.
    Oncotarget 2012;7:e42454
  7. Sprouting of substance P-expressing primary afferent central terminals and spinal micturition reflex NK1 receptor dependence after spinal cord injury.
    Authors: Zhang Et al.
    Am J Physiol Regul Integr Comp Physiol 2008;295:R2084
  8. TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats.
    Authors: Wang Et al.
    PLoS One 2008;294:R1517
  9. Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries.
    Authors: Gupta Et al.
    Naunyn Schmiedebergs Arch Pharmacol 2007;375:29
  10. Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-α-mediated apoptotic liver damage.
    Authors: Bang Et al.
    Br J Sports Med 2004;308:1174

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