Cat. No. 1145
Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl
Biological ActivityPotent 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 InformationSold with the permission of Merck, Sharpe and Dohme Ltd.
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 / Safety Data Sheet
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.
Liu et al (2013) TRPA1 controls inflammation and pruritogen responses in allergic contact dermatitis. FASEB J 27 3549. PMID: 23722916.
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.
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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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