SR 48692
Chemical Name: 2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid
Purity: ≥98%
Biological Activity
SR 48692 is a 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
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.
Background References
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Neurotensin and CRH interactions augment human mast cell activation.
Alysandratos K, Asadi S, Angelidou A, Zhang B, Sismanopoulos N, Yang H, Critchfield A, Theoharides T
PLoS ONE, 2012;7(11):e48934. -
Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor.
Gully et al.
Proc.Natl.Acad.Sci.USA, 1993;90:65 -
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.
Oury-Donat et al.
Br.J.Pharmacol., 1995;116:1899 -
The identification of nonpeptide neurotensin receptor partial agonists from the potent antagonist SR48692 using a calcium mobilization assay.
Thomas et al.
Bioorg.Med.Chem.Lett., 2009;19:1438
Product Datasheets
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Citations for SR 48692
The citations listed below are publications that use Tocris products. Selected citations for SR 48692 include:
7 Citations: Showing 1 - 7
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Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism.
Authors: Deluigi Et al.
Sci Adv 2020;7
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Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin.
Authors: Rouibi Et al.
PLoS One 2016;9:470
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Neurotensin Induces Presynaptic Depression of D2 DA Autoreceptor-Mediated Neurotransmission in Midbrain DArgic Neurons.
Authors: Piccart Et al.
J Neurosci 2015;35:11144
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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.
Authors: Toda Et al.
PLoS One 2014;9:e97421
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The neurotensin-HIF-1α-VEGFα axis orchestrates hypoxia, colonic inflammation, and intestinal angiogenesis.
Authors: Bakirtzi Et al.
Am J Pathol 2014;184:3405
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SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner.
Authors: Moody Et al.
PLoS One 2014;100:25
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Neurotensin and CRH interactions augment human mast cell activation.
Authors: Alysandratos Et al.
Life Sci 2012;7:e48934
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