Biological Activity
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.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.44 | 75 | |
| water | 17.15 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 685.86. 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 | 1.46 mL | 7.29 mL | 14.58 mL |
| 5 mM | 0.29 mL | 1.46 mL | 2.92 mL |
| 10 mM | 0.15 mL | 0.73 mL | 1.46 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.29 mL |
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References
References are publications that support the products' biological activity.
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
Keywords: SR 142948, supplier, potent, NT, receptor, antagonists, Receptors, Neurotensin, SR142948, Neurotensin, Receptors, Neurotensin, Receptors, Tocris Bioscience
