Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.74 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 587.07. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.7 mL | 8.52 mL | 17.03 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.41 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: SR 48692, supplier, SR48692, neurotensin, nts1, selective, antagonists, Neurotensin, Receptors, Neurotensin, Receptors, Tocris Bioscience
