Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewSR 48692
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[3.3.1.13,7]decane-2-carboxylic acid
Purity: ≥98% (HPLC)
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 |
| InChI Key | DYLJVOXRWLXDIG-UHFFFAOYSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for SR 48692
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.
View Related Products by Target
View Related Products by Product Action
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:
Alysandratos et al (2012) Neurotensin and CRH interactions augment human mast cell activation. Life Sci 7 e48934 PMID: 23155429
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
Moody et al (2014) SR48692 inhibits non-small cell lung cancer proliferation in an EGF receptor-dependent manner. PLoS One 100 25 PMID: 24496038
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
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.
Reviews for SR 48692
There are currently no reviews for this product. Be the first to review SR 48692 and earn rewards!
Have you used SR 48692?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
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
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.