Biological Activity
High affinity and potent ghrelin receptor inverse agonist (Ki values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq- and G13-dependent signaling pathways.
Technical Data
| M. Wt | 902.13 |
| Formula | C51H67N9O6 |
| Sequence |
KXFWLL (Modifications: X=D-1-Nal,Trp-4 = D-Trp, Leu-6 = C-terminal amide) |
| Storage | Store at -20°C |
| CAS Number | 1394288-22-2 |
| PubChem ID | 71453489 |
| InChI Key | NCMQVOQOKBIHPA-MHRDGXECSA-N |
| Smiles | [H]N[C@@H](CCCCN)C(=O)N[C@H](CC1=CC=CC2=C1C=CC=C2)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@H](CC1=CNC2=C1C=CC=C2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)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.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 902.13. 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 | 1.11 mL | 5.54 mL | 11.08 mL |
| 5 mM | 0.22 mL | 1.11 mL | 2.22 mL |
| 10 mM | 0.11 mL | 0.55 mL | 1.11 mL |
| 50 mM | 0.02 mL | 0.11 mL | 0.22 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Els et al (2012) An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor. J.Med.Chem. 55 7437 PMID: 22920150
M'Kadmi et al (2015) Agonism, antagonism, and inverse agonism bias at the ghrelin receptor signaling. J.Biol.Chem. 290 27021 PMID: 26363071
Keywords: K-(D-1-Nal)-FwLL-NH2, supplier, ghrelin, receptors, inverse, agonists, agonism, peptide, potent, high, affinity, Ghrelin, Receptors, Ghrelin, Receptors, Tocris Bioscience
