SR 48692

Pricing Availability   Qty
Description: Selective non-peptide NTS1 antagonist
Chemical Name: 2-[[[1-(7-Chloro-4-quinolinyl)-5-(2,6-dimethoxyphenyl)-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[,7]decane-2-carboxylic acid
Purity: ≥98% (HPLC)
Citations (7)
Literature (1)

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

SR 48692 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for SR 48692

M. Wt 587.07
Formula C32H31ClN4O5
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 146362-70-1
PubChem ID 119192
Smiles O=C(NC5(C(O)=O)C4CC(CC5C6)CC6C4)C2=NN(C(C3=C(OC)C=CC=C3OC)=C2)C1=C(C=CC(Cl)=C7)C7=NC=C1

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
DMSO 11.74 20

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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:

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

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

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

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

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Peptides Involved in Appetite Modulation Scientific Review

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.