L-733,060 hydrochloride

Cat. No. 1145

L-733,060 hydrochloride C20H19F6NO.HCl [148687-76-7]

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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.

Licensing Information

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

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

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.

Varty et al (2002) The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 27 371. PMID: 12225694.

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.

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

D'Amato et al (2015) A TDO2-AhR Signaling Axis Facilitates Anoikis Resistance and Metastasis in Triple-Negative Breast Cancer. Cancer Res 75 4651. PMID: 26363006.

García-Recio et al (2015) The Transmodulation of HER2 and EGFR by Substance P in Breast Cancer Cells Requires c-Src and Metalloproteinase Activation. PLoS One 10 e0129661. PMID: 26114632.

Backman et al (2014) Substance P reduces TNF-α-induced apoptosis in human tenocytes through NK-1 receptor stimulation. Mol Cancer Res 48 1414. PMID: 23996004.

Li et al (2013) Neurotransmitter substance P mediates pancreatic cancer perineural invasion via NK-1R in cancer cells. Am J Physiol Regul Integr Comp Physiol 11 294. PMID: 23345604.

Liu et al (2013) TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis. FASEB J 27 3549. PMID: 23722916.

Nassini et al (2012) Transient receptor potential ankyrin 1 channel localized to non-neuronal airway cells promotes non-neurogenic inflammation. Oncotarget 7 e42454. PMID: 22905134.

Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. PLoS One 294 R1517. PMID: 18337316.

Zhang et al (2008) Sprouting of substance P-expressing primary afferent central terminals and spinal micturition reflex NK1 receptor dependence after spinal cord injury. Am J Physiol Regul Integr Comp Physiol 295 R2084. PMID: 18945947.

Gupta et al (2007) Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol 375 29. PMID: 17295025.

Bang et al (2004) Neurokinin-1 receptor antagonists protect mice from CD95- and tumor necrosis factor-α-mediated apoptotic liver damage. Br J Sports Med 308 1174. PMID: 14617692.

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Keywords: L-733,060 hydrochloride, supplier, Potent, NK1, antagonists, Tachykinin, Receptors, Neurokinin, L733060, Tocris Bioscience, NK1 Receptor Antagonist products

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