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Biological Activity for SR 48692
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.
Compound Libraries for SR 48692
Technical Data for SR 48692
|Storage||Store at +4°C|
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 SR 48692
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for SR 48692
The following data is based on the product molecular weight 587.07. 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|
|0.2 mM||8.52 mL||42.58 mL||85.17 mL|
|1 mM||1.7 mL||8.52 mL||17.03 mL|
|2 mM||0.85 mL||4.26 mL||8.52 mL|
|10 mM||0.17 mL||0.85 mL||1.7 mL|
References for SR 48692
References are publications that support the biological activity of the product.
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
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
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
If you know of a relevant reference for SR 48692, please let us know.
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Keywords: SR 48692, SR 48692 supplier, SR48692, neurotensin, nts1, selective, antagonists, Neurotensin, Receptors, 3721, Tocris Bioscience
7 Citations for SR 48692
Citations are publications that use Tocris products. Selected citations for SR 48692 include:
Deluigi et al (2020) Complexes of the neurotensin receptor 1 with small-molecule ligands reveal structural determinants of full, partial, and inverse agonism. Sci Adv 7 PMID: 33571132
Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 DA Autoreceptor-Mediated Neurotransmission in Midbrain DArgic 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
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
Moody et al (2014) SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner. PLoS One 100 25 PMID: 24496038
Rouibi et al (2016) Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyrneurotensin. PLoS One 9 470 PMID: 26733785
Alysandratos et al (2012) Neurotensin and CRH interactions augment human mast cell activation. Life Sci 7 e48934 PMID: 23155429
Do you know of a great paper that uses SR 48692 from Tocris? Please let us know.
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Literature in this Area
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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.