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Submit ReviewL-733,060 hydrochloride
Description: Potent NK1 antagonist
Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
Purity: ≥99% (HPLC)
Biological Activity for L-733,060 hydrochloride
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.
Technical Data for L-733,060 hydrochloride
| M. Wt | 439.83 |
| Formula | C20H19F6NO.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for L-733,060 hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 21.99 | 50 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 will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.55 mL | 22.74 mL | 45.47 mL |
| 2.5 mM | 0.91 mL | 4.55 mL | 9.09 mL |
| 5 mM | 0.45 mL | 2.27 mL | 4.55 mL |
| 25 mM | 0.09 mL | 0.45 mL | 0.91 mL |
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Product Datasheets for L-733,060 hydrochloride
References for L-733,060 hydrochloride
References are publications that support the biological activity of the product.
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
Varty et al (2002) The gerbil elevated plus-maze II: anxiolytic-like effects of selective neurokinin NK1 receptor antagonists. Neuropsychopharmacology 27 371 PMID: 12225694
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
If you know of a relevant reference for L-733,060 hydrochloride, please let us know.
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Keywords: L-733,060 hydrochloride, L-733,060 hydrochloride supplier, Potent, NK1, antagonists, Tachykinin, Receptors, Neurokinin, L733060, Receptor, 1145, Tocris Bioscience
15 Citations for L-733,060 hydrochloride
Citations are publications that use Tocris products. Selected citations for L-733,060 hydrochloride include:
Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. PLoS One 294 R1517 PMID: 18337316
Muschter et al (2019) Sensory Neuropeptides and their Receptors Participate in Mechano-Regulation of Murine Macrophages. Int J Mol Sci 20 PMID: 30682804
Khasabov et al (2017) Hyperalgesia and sensitization of dorsal horn neurons following activation of NK-1 receptors in the rostral ventromedial medulla. J Neurophysiol 118 2727 PMID: 28794197
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
Liu et al (2013) TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis. FASEB J 27 3549 PMID: 23722916
Fong et al (2017) The effects of substance P and acetylcholine on human tenocyte proliferation converge mechanistically via TGF-β1. PLoS One 12 e0174101 PMID: 28301610
Nassini et al (2010) 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. FASEB J 24 4904 PMID: 20720158
Sloniecka et al (2016) Substance P Enhances Keratocyte Migration and Neutrophil Recruitment through Interleukin-8. Mol Pharmacol 89 215 PMID: 26646648
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
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
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
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
Gupta et al (2007) Pharmacological characterisation of capsaicin-induced relaxations in human and porcine isolated arteries. Naunyn Schmiedebergs Arch Pharmacol 375 29 PMID: 17295025
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
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
Depression Poster
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.