Biological Activity
Potent neuropeptide Y (NPY) Y1 receptor antagonist (pA2 = 10 and 10.5 at rY1 and hY1, receptors respectively). Also a potent and selective NPY Y4 receptor agonist (pEC50 values are 6.0, 8.6 and 6.1 for rY2, hY4 and rY5 receptors respectively). Suppresses food intake in rats in vivo. Also has affinity for neuropeptide FF (NPFF) receptors in vitro (Ki = 43-73 nM).
Technical Data
| M. Wt | 2352.77 |
| Formula | C110H170N34O24 |
| Sequence |
IEPXYRLRY IEPXYRLRY* (Modifications: X = Dpr, Amide Bridge = 2 - 4*, 4 - 2*, Tyr-9 = C-terminal amide) |
| Storage | Desiccate at -20°C |
| CAS Number | 158859-98-4 |
| PubChem ID | 24868178 |
| InChI Key | RJRBRCCJETZJLT-GSICZYLSSA-N |
| Smiles | [H]N[C@@H]([C@@H](C)CC)C(=O)N[C@H]1CCC(=O)NCC(NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCC(=O)NCC(NC(=O)[C@@H]2CCCN2C1=O)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=O)NC(=O)[C@@H](N[H])[C@@H](C)CC)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CC=C(O)C=C1)C(N)=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.
Preparing Stock Solutions
The following data is based on the product molecular weight 2352.77. 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 | 0.43 mL | 2.13 mL | 4.25 mL |
| 5 mM | 0.09 mL | 0.43 mL | 0.85 mL |
| 10 mM | 0.04 mL | 0.21 mL | 0.43 mL |
| 50 mM | 0.01 mL | 0.04 mL | 0.09 mL |
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References
References are publications that support the products' biological activity.
Ishihara et al (1998) A potent neuropeptide Y antagonist, 1229U91, suppressed spontaneous food intake in Zucker fatty rats. Am.J.Physiol. 274 R1500 PMID: 9612420
Mollereau et al (2001) Agonist and antagonist activities on human NPFF2 receptors of the NPY ligands GR231118 and BIBP3226. Br.J.Pharmacol. 133 1 PMID: 11325787
Parker et al (1998) GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur.J.Pharmacol. 349 97 PMID: 9669502
Keywords: GR 231118, supplier, NPFF, receptor, ligands, NPY, Y1, antagonists, Y4, agonists, Neuropeptide, FF, GR231118, npffr1, npffr2, npff1, npff2, GW1229, 1229, U91, neuropeptides, 1229U91, GW, 1229, NPY, Receptors, Neuropeptide, FF/AF, Receptors, NPY, Receptors, Tocris Bioscience
