Chemical Name:N-[(1S)-4-[(Aminoiminomethyl)amino]-1-[[[2-(3,5-dioxo-1,2-diphenyl-1,2,4-triazolidin-4-yl)ethyl]amino]carbonyl]butyl]-1-[2-[4-(6,11-dihydro-6-oxo-5H-dibenz[b,e]azepin-11-yl)-1-piperazinyl]-2-oxoethyl]-cyclopentaneacetamide
Purity: ≥98% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
Biological Activity
Potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor (IC50 = 15 nM). Displays > 650-fold selectivity over Y1, Y4 and Y5 receptors. 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
67.2
75
ethanol
23.55
25
Preparing Stock Solutions
The following data is based on the product molecular weight 896.06. 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
1.12 mL
5.58 mL
11.16 mL
5 mM
0.22 mL
1.12 mL
2.23 mL
10 mM
0.11 mL
0.56 mL
1.12 mL
50 mM
0.02 mL
0.11 mL
0.22 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.
Doodset al (1999) BIIE0246: a selective and high affinity neuropeptide Y Y2 receptor antagonist. Eur.J.Pharmacol. 384 R3 PMID: 10611450
Dumontet al (2000) BIIE0246, a potent and highly selective non-peptide neuropeptide Y Y2 receptor antagonist. Br.J.Pharmacol. 129 1075 PMID: 10725255
Malmstrom
(2001) Vascular pharmacology of BIIE0246, the first selective non-peptide neuropeptide Y Y2 receptor antagonist, in vivo. Br.J.Pharmacol. 133 1073 PMID: 11487518