Biological Activity
Ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo.
Compound Libraries
YIL 781 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 445.96 |
| Formula | C24H28FN3O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 875258-85-8 |
| PubChem ID | 74889155 |
| InChI Key | QQGRMONBDBMLSP-FERBBOLQSA-N |
| Smiles | O=C2C1=CC(OC4=CC=C(F)C=C4)=CC=C1N=C(C)N2C[C@@H]3CN(C(C)C)CCC3.Cl |
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 | 44.6 | 100 | |
| ethanol | 44.6 | 100 | |
| water | 44.6 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 445.96. 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 | 2.24 mL | 11.21 mL | 22.42 mL |
| 5 mM | 0.45 mL | 2.24 mL | 4.48 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.24 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Esler et al (2007) Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology 148 5175 PMID: 17656463
Moran and Dailey (2009) Gut peptides: targets for antiobesity drug development? Endocrinology 150 2526 PMID: 19372201
Keywords: YIL 781, supplier, YIL781, YIL, 781, hydrochloride, ghrelin, receptors, antagonists, GHS-R1a, GHSR, Ghrelin, Receptors, Ghrelin, Receptors, Tocris Bioscience
