Biological Activity
Potent, orally active ghrelin receptor (GHS-R1a) agonist (Ki = 50 nM at human recombinant GHS-R1a). Stimulates GH release from rat pituitary cells with an EC50 value of 2.7 nM. Induces hyperphagia and adiposity in lean rats, but not in leptin signaling-deficient ZDF rats.
Technical Data
| M. Wt | 586.73 |
| Formula | C32H40N4O3.½C4H4O4 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 242143-80-2 |
| PubChem ID | 11981159 |
| InChI Key | YQDJPWXYLLPOPW-LWTUVRFUSA-N |
| Smiles | [H]OC(=O)C=CC(=O)O[H].CNC(=O)[C@@H](CC1=CC=CC=C1)N(C)C(=O)[C@@H](CC1=CC2=CC=CC=C2C=C1)N(C)C(=O)C=CCC(C)(C)N.CNC(=O)[C@@H](CC1=CC=CC=C1)N(C)C(=O)[C@@H](CC1=CC2=CC=CC=C2C=C1)N(C)C(=O)C=CCC(C)(C)N |
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 | 58.67 | 100 | |
| water | 5.29 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 586.73. 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 | 1.7 mL | 8.52 mL | 17.04 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.41 mL |
| 10 mM | 0.17 mL | 0.85 mL | 1.7 mL |
| 50 mM | 0.03 mL | 0.17 mL | 0.34 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hansen et al (1999) Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur.J.Endocrinol. 141 180 PMID: 10427162
Holm et al (2004) Adipogenic and orexigenic effects of the ghrelin-receptor ligand tabimorelin are diminished in leptin-signalling-deficient ZDF rats. Eur.J.Pharmacol. 150 893 PMID:
Keywords: Tabimorelin hemifumarate, supplier, Potent, orally, active, ghrelin, receptor, agonists, GHS-R1a, Receptors, Growth, Hormone, Secretagog, 1a, NN703, NN, 703, Ghrelin, Receptors, Ghrelin, Receptors, Tocris Bioscience
