L-733,060 hydrochloride

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Cat.No. 1145 - L-733,060 hydrochloride | C20H19F6NO.HCl | CAS No. 148687-76-7
Description: Potent NK1 antagonist
Chemical Name: (2S,3S)-3-[[3,5-bis(Trifluoromethyl)phenyl]methoxy]-2-phenylpiperidine hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (10)
Literature

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
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 21.99 50mM with gentle warming

Preparing Stock Solutions

The following data is based on the product molecular weight 439.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.27 mL 11.37 mL 22.74 mL
5 mM 0.45 mL 2.27 mL 4.55 mL
10 mM 0.23 mL 1.14 mL 2.27 mL
50 mM 0.05 mL 0.23 mL 0.45 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: Potent NK1 antagonists Tachykinin Receptors Neurokinin L733060 NK1 Receptor

10 Citations for L-733,060 hydrochloride

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

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

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

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

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

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

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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