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Submit ReviewSR 142948
Description: Highly potent NTS receptor antagonist
Chemical Name: 2-[[[5-(2,6-Dimethoxyphenyl)-1-[4-[[[3-(dimethylamino)propyl]methylamino]carbonyl]-2-(1-methylethyl)phenyl]-1H-pyrazol-3-yl]carbonyl]amino]-tricyclo[3.3.1.13,7]decane-2-carboxylic acid
Purity: ≥97% (HPLC)
Biological Activity for SR 142948
SR 142948 is a potent non-peptide neurotensin (NT) receptor antagonist that binds with high affinity (IC50 = 0.32 - 3.96 nM; Ki < 10 nM). Attenuates amphetamine-induced hyperactivity and is orally active in vivo.
Compound Libraries for SR 142948
SR 142948 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for SR 142948
| M. Wt | 685.86 |
| Formula | C39H51N5O6 |
| Storage | Store at +4°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 184162-64-9 |
| PubChem ID | 5311451 |
| InChI Key | LWULHXVBLMWCHO-UHFFFAOYSA-N |
| Smiles | COC1=CC=CC(OC)=C1C1=CC(=NN1C1=C(C=C(C=C1)C(=O)N(C)CCCN(C)C)C(C)C)C(=O)NC1(C2CC3CC(C2)CC1C3)C(O)=O |
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 142948
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.44 | 75 | |
| water | 17.15 | 25 |
Preparing Stock Solutions for SR 142948
The following data is based on the product molecular weight 685.86. 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 |
|---|---|---|---|
| 0.75 mM | 1.94 mL | 9.72 mL | 19.44 mL |
| 3.75 mM | 0.39 mL | 1.94 mL | 3.89 mL |
| 7.5 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 37.5 mM | 0.04 mL | 0.19 mL | 0.39 mL |
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Product Datasheets for SR 142948
References for SR 142948
References are publications that support the biological activity of the product.
Gully et al (1997) Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J.Pharmacol.Exp.Ther. 280 802 PMID: 9023294
Quere et al (1998) X-ray structural characterization of SR 142948, a novel potent synthetic neurotensin receptor antagonist. Bioorg.Med.Chem.Lett. 8 653 PMID: 9871577
Marie-Claire et al (2008) Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice. Neuropharmacology 54 1107 PMID: 18410947
If you know of a relevant reference for SR 142948, please let us know.
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Keywords: SR 142948, SR 142948 supplier, potent, NT, receptor, antagonists, Receptors, Neurotensin, SR142948, 2309, Tocris Bioscience
4 Citations for SR 142948
Citations are publications that use Tocris products. Selected citations for SR 142948 include:
Rouibi et al (2016) Ventral Midbrain NTS1 Receptors Mediate Conditioned Reward Induced by the Neurotensin Analog, D-Tyr[11]neurotensin. J Cereb Blood Flow Metab 9 470 PMID: 26733785
Yin et al (2008) Neurotensin reduces glutamatergic transmission in the dorsolateral striatum via retrograde endocannabinoid signaling. Neuropharmacology 54 79 PMID: 17675102
Piccart et al (2015) Neurotensin Induces Presynaptic Depression of D2 DA Autoreceptor-Mediated Neurotransmission in Midbrain DArgic Neurons. J Neurosci 35 11144 PMID: 26245975
Olszewski-Hamilton and Hamilton (2011) Dependence of Relative Expression of NTR1 and EGFR on Cell Density and Extracellular pH in Human Pancreatic Cancer Cell Lines. Cancers (Basel) 3 182 PMID: 24212612
Do you know of a great paper that uses SR 142948 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!
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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.