L-733,060 hydrochloride

  ( 12 citations )    
Product Datasheet
Catalog Number:1145
Chemical Name:(2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
Product Details
Citations (12)
Supplemental Products
Reviews
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.
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Citations:

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

12 Citations: Showing 1 - 10
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  1. The effects of substance P and acetylcholine on human tenocyte proliferation converge mechanistically via TGF-β1.
    Authors: Fong Et al.
    PLoS One  2017;12:e0174101
  2. 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
  3. 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
  4. 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
  5. TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis.
    Authors: Liu Et al.
    FASEB J  2013;27:3549
  6. 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
  7. Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation.
    Authors: Nassini Et al.
    Oncotarget  2012;7:e42454
  8. Acetaminophen, via its reactive metabolite N-acetyl-p-benzo-quinoneimine and transient receptor potential ankyrin-1 stimulation, causes neurogenic inflammation in the airways and other tissues in rodents.
    Authors: Nassini Et al.
    FASEB J  2010;24:4904
  9. 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
  10. TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats.
    Authors: Wang Et al.
    PLoS One  2008;294:R1517
  11. Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries.
    Authors: Gupta Et al.
    Naunyn Schmiedebergs Arch Pharmacol  2007;375:29
  12. 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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