SR 48692

Cat. No. 3721

SR 48692 C32H31ClN4O5 [146362-70-1]

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Chemical Name: 2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[,7]decane-2-carboxylic acid

Biological Activity

Neurotensin antagonist; selective for NTS1 over NTS2 (apparent affinity, Ke, is 36 nM for NTS1). Competitively inhibits binding of [125I]-neurotensin to HT29 and N1E115 cell membranes (IC50 values are 15.3 and 20.4 nM respectively). Orally bioavailable.

Technical Data

Soluble to 20 mM in DMSO
>98 %
Store at +4°C

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

Certificate of Analysis: View current batch
Safety Data Sheet: View Safety Data Sheet

Thomas et al (2009) The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay. Bioorg.Med.Chem.Lett. 19 1438. PMID: 19195889.

Oury-Donat et al (1995) Characterization of the effect of SR48692 on inositol monophosphate, cyclic GMP and cyclic AMP responses linked to neurotensin receptor activation in neuronal and non-neuronal cells. Br.J.Pharmacol. 116 1899. PMID: 8528577.

Gully et al (1993) Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc.Natl.Acad.Sci.USA 90 65. PMID: 8380498.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for SR 48692 include:

Rouibi et al (2016) Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin. PLoS One 9 470. PMID: 26733785.

Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 Dopamine Autoreceptor-Mediated Neurotransmission in Midbrain Dopaminergic Neurons. J Neurosci 35 11144. PMID: 26245975.

Bakirtzi et al (2014) The neurotensin-HIF-1α-VEGFα axis orchestrates hypoxia, colonic inflammation, and intestinal angiogenesis. Am J Pathol 184 3405. PMID: 25307345.

Moody et al (2014) SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner. PLoS One 100 25. PMID: 24496038.

Toda et al (2014) Maternal separation enhances conditioned fear and decreases the mRNA levels of the neurotensin receptor 1 gene with hypermethylation of this gene in the rat amygdala. PLoS One 9 e97421. PMID: 24831231.

Alysandratos et al (2012) Neurotensin and CRH interactions augment human mast cell activation. Life Sci 7 e48934. PMID: 23155429.

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Keywords: SR 48692, supplier, SR48692, neurotensin, nts1, selective, antagonists, Tocris Bioscience, Neurotensin Receptor Antagonist products

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