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
Technical Data
Solubility
Calculators
Datasheets
References
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.
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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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Gullyet al (1997) Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J.Pharmacol.Exp.Ther. 280 802 PMID: 9023294
Quereet 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-Claireet al (2008) Effects of the selective neurotensin antagonist SR 142948A on 3,4-methylenedioxymethamphetamine-induced behaviours in mice. Neuropharmacology 54 1107 PMID: 18410947