L-733,060 hydrochloride

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1145/10
1145/50
L-733,060 hydrochloride | CAS No. 148687-76-7 | NK1 Receptor Antagonists
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Description: Potent NK1 antagonist

Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride

Purity: ≥99%

Product Details
Citations (15)
Supplemental Products
Reviews

Biological Activity

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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of Merck, Sharpe and Dohme Ltd.

Product Datasheets

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Citations for L-733,060 hydrochloride

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

15 Citations: Showing 1 - 10

  1. Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages.
    Authors: Muschter Et al.
    Int J Mol Sci  2019;20
  2. 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
  3. Hyperalgesia and sensitization of dorsal horn neurons following activation of NK-1 receptors in the rostral ventromedial medulla.
    Authors: Khasabov Et al.
    J Neurophysiol  2017;118:2727
  4. Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8.
    Authors: Sloniecka Et al.
    Mol Pharmacol  2016;89:215
  5. 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
  6. 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
  7. 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
  8. TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis.
    Authors: Liu Et al.
    FASEB J  2013;27:3549
  9. 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
  10. Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation.
    Authors: Nassini Et al.
    Oncotarget  2012;7:e42454

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